BR112015003041A2 - Intermediário para síntese de 1-(2-desóxi-2-fluoro-4 -tio-\beta-d-arabinofuranosil)citosina , intermediário para síntese de tionucleosídeo , e métodos para produzir estes intermediários - Google Patents

Intermediário para síntese de 1-(2-desóxi-2-fluoro-4 -tio-\beta-d-arabinofuranosil)citosina , intermediário para síntese de tionucleosídeo , e métodos para produzir estes intermediários

Info

Publication number
BR112015003041A2
BR112015003041A2 BR112015003041-6A BR112015003041A BR112015003041A2 BR 112015003041 A2 BR112015003041 A2 BR 112015003041A2 BR 112015003041 A BR112015003041 A BR 112015003041A BR 112015003041 A2 BR112015003041 A2 BR 112015003041A2
Authority
BR
Brazil
Prior art keywords
synthesis
dexyx
arabinofuranosil
thionucleoside
intermediaries
Prior art date
Application number
BR112015003041-6A
Other languages
English (en)
Japanese (ja)
Other versions
BR112015003041B1 (pt
Inventor
Nakamura Kouki
Shimamura Satoshi
Imoto Junichi
Takahashi Motomasa
Watanabe Katsuyuki
Wada Kenji
Fujino Yuuta
Matsumoto Takuya
Takahashi Makoto
Okada Hideki
Yamane Takehiro
Ito Takayuki
Original Assignee
Fujifilm Corporation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Fujifilm Corporation filed Critical Fujifilm Corporation
Publication of BR112015003041A2 publication Critical patent/BR112015003041A2/pt
Publication of BR112015003041B1 publication Critical patent/BR112015003041B1/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30Hetero atoms other than halogen
    • C07D333/32Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/32Oximes
    • C07C251/34Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C251/36Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atoms of the oxyimino groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/38Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atoms of the oxyimino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a saturated carbon skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B53/00Asymmetric syntheses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C249/00Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C249/04Preparation of compounds containing nitrogen atoms doubly-bound to a carbon skeleton of oximes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/32Oximes
    • C07C251/34Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C251/36Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atoms of the oxyimino groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/40Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atoms of the oxyimino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/26Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids
    • C07C303/28Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of esters of sulfonic acids by reaction of hydroxy compounds with sulfonic acids or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/72Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00Compounds having —CHO groups
    • C07C47/02Saturated compounds having —CHO groups bound to acyclic carbon atoms or to hydrogen
    • C07C47/19Saturated compounds having —CHO groups bound to acyclic carbon atoms or to hydrogen containing hydroxy groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C47/00Compounds having —CHO groups
    • C07C47/20Unsaturated compounds having —CHO groups bound to acyclic carbon atoms
    • C07C47/277Unsaturated compounds having —CHO groups bound to acyclic carbon atoms containing ether groups, groups, groups, or groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/28Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/29Preparation of carboxylic acid esters by modifying the hydroxylic moiety of the ester, such modification not being an introduction of an ester group by introduction of oxygen-containing functional groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C68/00Preparation of esters of carbonic or haloformic acids
    • C07C68/06Preparation of esters of carbonic or haloformic acids from organic carbonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
    • C07C69/28Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with dihydroxylic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/612Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a six-membered aromatic ring in the acid moiety
    • C07C69/618Esters of carboxylic acids having a carboxyl group bound to an acyclic carbon atom and having a six-membered aromatic ring in the acid moiety having unsaturation outside the six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/78Benzoic acid esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • C07C69/84Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring
    • C07C69/92Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/96Esters of carbonic or haloformic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30Hetero atoms other than halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • C07F7/1872Preparation; Treatments not provided for in C07F7/20
    • C07F7/188Preparation; Treatments not provided for in C07F7/20 by reactions involving the formation of Si-O linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00Processes for the preparation of sugar derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/04Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02Acyclic radicals, not substituted by cyclic structures
    • C07H15/04Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18Acyclic radicals, substituted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/203Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/067Pyrimidine radicals with ribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • C07H19/073Pyrimidine radicals with 2-deoxyribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H23/00Compounds containing boron, silicon, or a metal, e.g. chelates, vitamin B12
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H5/00Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
    • C07H5/02Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H5/00Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
    • C07H5/08Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to sulfur, selenium or tellurium
    • C07H5/10Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium to sulfur, selenium or tellurium to sulfur
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04Carbocyclic radicals
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
BR112015003041-6A 2012-08-13 2013-08-13 Métodos de produção de compostos intermediários para síntese de 1-(2-desóxi-2-fluoro-4- tio-ss-d-arabinofuranosil)citosina e tionucleosídeo BR112015003041B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2012-179380 2012-08-13
JP2012179380 2012-08-13
JP2013012693 2013-01-25
JP2013-012693 2013-01-25
PCT/JP2013/071871 WO2014027658A1 (ja) 2012-08-13 2013-08-13 1-(2-デオキシ-2-フルオロ-4-チオ-β-D-アラビノフラノシル)シトシンの合成中間体およびチオヌクレオシドの合成中間体ならびにそれらの製造法

Publications (2)

Publication Number Publication Date
BR112015003041A2 true BR112015003041A2 (pt) 2018-05-29
BR112015003041B1 BR112015003041B1 (pt) 2022-07-26

Family

ID=50685606

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015003041-6A BR112015003041B1 (pt) 2012-08-13 2013-08-13 Métodos de produção de compostos intermediários para síntese de 1-(2-desóxi-2-fluoro-4- tio-ss-d-arabinofuranosil)citosina e tionucleosídeo

Country Status (24)

Country Link
US (4) US9221865B2 (pt)
EP (2) EP2883866B1 (pt)
JP (2) JP5970550B2 (pt)
KR (3) KR101770248B1 (pt)
CN (2) CN107011168B (pt)
AU (1) AU2013303534B2 (pt)
BR (1) BR112015003041B1 (pt)
CA (1) CA2880794C (pt)
CY (1) CY1121617T1 (pt)
DK (1) DK2883866T3 (pt)
ES (1) ES2718307T3 (pt)
HK (1) HK1208436A1 (pt)
HR (1) HRP20190572T1 (pt)
HU (1) HUE044412T2 (pt)
IL (1) IL237086B (pt)
LT (1) LT2883866T (pt)
MX (1) MX2015001935A (pt)
PL (1) PL2883866T3 (pt)
PT (1) PT2883866T (pt)
RS (1) RS58568B1 (pt)
RU (1) RU2633355C2 (pt)
SI (1) SI2883866T1 (pt)
TW (1) TWI603966B (pt)
WO (1) WO2014027658A1 (pt)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI637963B (zh) * 2012-03-28 2018-10-11 富士軟片股份有限公司 1-(2-脫氧-2-氟-4-硫-β-D-***呋喃糖基)胞嘧啶之鹽
PL2883866T3 (pl) 2012-08-13 2019-07-31 Fujifilm Corporation Produkt pośredni do syntezy 1-(2-deoksy-2-fluoro-4-tio-beta-d-arabinofuranosylo)cytozyny, produkt pośredni do syntezy tionukleozydu i sposoby otrzymywania tych produktów pośrednich
JP6175553B2 (ja) * 2014-02-18 2017-08-09 富士フイルム株式会社 チオラン骨格型糖化合物の製造方法およびチオラン骨格型糖化合物
JP6351107B2 (ja) * 2014-02-18 2018-07-04 富士フイルム株式会社 チオラン骨格型糖化合物の製造方法およびチオラン骨格型糖化合物
JP6204223B2 (ja) 2014-02-19 2017-09-27 富士フイルム株式会社 チオピラノース化合物等の製造方法
JP6245527B2 (ja) * 2014-03-24 2017-12-13 富士フイルム株式会社 チオラン環もしくはチアン環骨格を有する化合物の製造方法
JP6253169B2 (ja) * 2014-09-24 2017-12-27 富士フイルム株式会社 環状ヘミアセタール化合物の製造方法
TWI678373B (zh) 2014-10-31 2019-12-01 日商富士軟片股份有限公司 硫代核苷衍生物或其鹽及醫藥組合物
JP6450356B2 (ja) 2016-02-29 2019-01-09 富士フイルム株式会社 液状医薬製剤
JP6719369B2 (ja) * 2016-05-13 2020-07-08 富士フイルム株式会社 2’−フルオロ−5−メチル−4’−チオアラビノウリジンの製造方法及びその一部の工程を含む方法
MX2019002430A (es) 2016-08-31 2019-07-04 Fujifilm Corp Agente antitumoral, mejorador del efecto antitumoral, y kit antitumoral.
CN110573521B (zh) * 2017-06-29 2023-04-21 四川科伦博泰生物医药股份有限公司 4’-硫代核苷的新型化合物的制备方法和此制备方法中的中间体
CA3089728C (en) 2018-01-29 2023-01-10 Fujifilm Corporation Antitumor agent for biliary tract cancer and method for treating biliary tract cancer
WO2019176984A1 (ja) 2018-03-13 2019-09-19 富士フイルム株式会社 抗腫瘍剤、抗腫瘍効果増強剤及び抗腫瘍用キット
WO2019204637A1 (en) * 2018-04-19 2019-10-24 Southern Research Institute 4'-thio-nucleotide and -nucleoside prodrugs for the treatment of cancer
WO2020031179A1 (en) * 2018-08-06 2020-02-13 Beetlebung Pharma Ltd. Methods for synthesis of cannabinoid compounds
WO2023008511A1 (ja) 2021-07-29 2023-02-02 富士フイルム株式会社 Bap1およびpbrm1の少なくとも1つの機能低下を有する腫瘍に対する医薬組成物および抗腫瘍剤
CN114380877B (zh) * 2022-01-26 2023-03-28 和德化学(苏州)有限公司 一种2’-脱氧-2’-β-氟-4’-叠氮胞苷的制备方法

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3116282A (en) 1960-04-27 1963-12-31 Upjohn Co Pyrimidine nucleosides and process
US3243425A (en) 1962-10-29 1966-03-29 Purdue Research Foundation Novel sulfur-containing compounds
JPS53119810A (en) 1977-03-25 1978-10-19 Mitsubishi Chem Ind Ltd Preparation of aldehyde chloride
US4211773A (en) 1978-10-02 1980-07-08 Sloan Kettering Institute For Cancer Research 5-Substituted 1-(2'-Deoxy-2'-substituted-β-D-arabinofuranosyl)pyrimidine nucleosides
US4220774A (en) 1978-10-26 1980-09-02 Omnium Chimique Vincadifformine synthesis process
JPS5692239A (en) 1979-12-27 1981-07-25 Sagami Chem Res Center Preparation of 5-oxohexyl compound
US4803272A (en) 1987-02-24 1989-02-07 E. I. Du Pont De Nemours And Company S-modified adenosyl-1,8-diamino-3-thiooctane derivatives
IE74701B1 (en) 1989-10-04 1997-07-30 Univ Birmingham Further antiviral pyrimidine nucleosides
DK0494956T3 (da) 1989-10-06 1996-04-22 Cosan Chem Corp Aminocarboxylatsalte som korrosionsinhibitorer i overtræk
SE9003151D0 (sv) 1990-10-02 1990-10-02 Medivir Ab Nucleoside derivatives
JP3138834B2 (ja) 1991-12-26 2001-02-26 生化学工業株式会社 フコピラノース類縁体の製造方法およびその合成中間化合物
GB9218810D0 (en) 1992-09-04 1992-10-21 Univ Birmingham Antiviral pyrimidine nucleosides
WO1996001834A1 (fr) 1994-07-12 1996-01-25 Yamasa Corporation 2'-desoxy-2'-(methylidene substitue ou non substitue)-4'-thionucleoside
JPH0853490A (ja) 1994-08-09 1996-02-27 Yamasa Shoyu Co Ltd 2’−デオキシ−2’,2’−ジハロゲノ−4’−チオヌクレオシド
WO1997038001A1 (fr) 1996-04-09 1997-10-16 Yamasa Corporation 1-(2-DESOXY-2-FLUORO-4-THIO-β-D-ARABINOFURANOSYL)CYTOSINES
JP4202327B2 (ja) 1996-04-09 2008-12-24 ヤマサ醤油株式会社 1−(2−デオキシ−2−フルオロ−4−チオ−β−D−アラビノフラノシル)シトシン
WO1997037993A1 (fr) 1996-04-09 1997-10-16 Yamasa Corporation DERIVES DE 9-(2-DESOXY-2-FLUORO-4-THIO-β-D-ARABINOFURANOSYL)PURINE
US7875733B2 (en) 2003-09-18 2011-01-25 Isis Pharmaceuticals, Inc. Oligomeric compounds comprising 4′-thionucleosides for use in gene modulation
HUP9601756A3 (en) 1996-06-25 1999-05-28 Richter Gedeon Vegyeszet New anticoagulant glycosides and pharmaceutical compositions containing them
JP4087471B2 (ja) * 1997-03-31 2008-05-21 大日本印刷株式会社 表面プラズモン共鳴バイオセンサー用測定チップ及びその製造方法
HUP9702348A3 (en) 1997-12-04 2000-12-28 Richter Gedeon Vegyeszet New anticoagulant glycosides and pharmaceutical conew anticoagulant glycosides and pharmaceutical compositions containing them mpositions containing them
WO1999043690A1 (fr) * 1998-02-25 1999-09-02 Rational Drug Design Laboratories Compose de l-4'-arabinofuranonucleoside et composition medicinale le contenant
AU2001240098A1 (en) 2000-03-08 2001-09-17 Southern Research Institute 4'-thio-l-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof
KR100426030B1 (ko) 2000-07-22 2004-04-03 (주) 한켐 락톤계 당화합물에서의 키랄성 전환방법
TWI247609B (en) * 2001-01-23 2006-01-21 Nihon Mediphysics Co Ltd Agent for diagnosis of tissue proliferation activity or the treatment of proliferative disease
GB0114286D0 (en) * 2001-06-12 2001-08-01 Hoffmann La Roche Nucleoside Derivatives
BR0210594A (pt) 2001-06-22 2005-11-01 Pharmasset Ltd (beta)-d ou (beta)-l-3-halonucleosìdeo
JP2003172990A (ja) 2001-08-03 2003-06-20 Fuji Photo Film Co Ltd ハロゲン化銀乳剤及びハロゲン化銀写真感光材料
BR0310006A (pt) 2002-08-09 2005-02-15 Taisho Pharmaceutical Co Ltd Derivados de 5-tio-beta-d-glicopiranosìdeo de arila e agentes terapêuticos para diabetes contendo os mesmos
AU2003200960B2 (en) 2002-09-18 2005-01-06 Mackinnon, Sebastian Mr System for Ordering, Tracking and Payment of Goods and Services
CA2525099A1 (en) 2003-05-12 2004-11-25 Purdue Research Foundation Cytotoxic indeno and isoindoloisoquinolones
EP1630157A4 (en) 2003-05-28 2007-05-23 Japan Tobacco Inc ANTAGONIST OF CASR
JPWO2004106352A1 (ja) 2003-05-29 2006-07-20 大正製薬株式会社 アルドヘキソピラノース中間体の製造法
GB0317009D0 (en) 2003-07-21 2003-08-27 Univ Cardiff Chemical compounds
TW200637839A (en) 2005-01-07 2006-11-01 Taisho Pharmaceutical Co Ltd 1-thio-d-glucitol derivatives
ATE516026T1 (de) 2005-02-21 2011-07-15 Shionogi & Co Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung
JP2006335737A (ja) * 2005-06-03 2006-12-14 Ihara Nikkei Kagaku Kogyo Kk ベンゾ[c]ヘテロ5員環化合物の製造方法
WO2007056596A2 (en) 2005-11-09 2007-05-18 Wayne State University Phosphoramidate derivatives of fau
WO2007068113A1 (en) 2005-12-16 2007-06-21 Mcgill University 4'-thioarabinonucleotide-containing oligonucleotides, compounds and methods for their preparation and uses thereof
CN100513395C (zh) * 2006-04-17 2009-07-15 中国科学院化学研究所 一种制备多羟基环状硝酮的方法
JP5320284B2 (ja) 2006-05-03 2013-10-23 キメリクス,インコーポレーテッド 抗ウイルス性または抗増殖性のホスホネート、ヌクレオシドホスホネートおよびヌクレオシドホスフェートの代謝安定性アルコキシアルキルエステル
CN101200463B (zh) 2007-12-11 2011-06-22 复旦大学 全酰化-4-硫代-d-核糖及其制备方法
US8859589B2 (en) 2008-03-12 2014-10-14 Southern Research Institute Use of 4′-thio-2′-deoxynucleosides as anti orthopoxvirus agents
CN101880287B (zh) * 2009-05-05 2012-07-25 上海医药工业研究院 一类四氢噻吩核苷类似物的中间体化合物及其制备方法
CN102656154B (zh) 2009-12-18 2014-04-09 天秤医药股份有限公司 用于制备取代的1-O-酰基-2-脱氧-2-氟-4-硫代-β-D-***呋喃糖的方法
GB201016855D0 (en) 2010-10-06 2010-11-17 Nucana Biomed Ltd Chemical compounds
TWI637963B (zh) 2012-03-28 2018-10-11 富士軟片股份有限公司 1-(2-脫氧-2-氟-4-硫-β-D-***呋喃糖基)胞嘧啶之鹽
PL2883866T3 (pl) 2012-08-13 2019-07-31 Fujifilm Corporation Produkt pośredni do syntezy 1-(2-deoksy-2-fluoro-4-tio-beta-d-arabinofuranosylo)cytozyny, produkt pośredni do syntezy tionukleozydu i sposoby otrzymywania tych produktów pośrednich
TWI678373B (zh) 2014-10-31 2019-12-01 日商富士軟片股份有限公司 硫代核苷衍生物或其鹽及醫藥組合物
CN109553651B (zh) 2015-04-03 2021-08-06 四川科伦博泰生物医药股份有限公司 4’-硫代核苷的新型化合物及其制备方法、药物组合物和应用

Also Published As

Publication number Publication date
US10570112B2 (en) 2020-02-25
US20150152131A1 (en) 2015-06-04
KR20150036544A (ko) 2015-04-07
SI2883866T1 (sl) 2019-07-31
JP5970550B2 (ja) 2016-08-17
CN107011168A (zh) 2017-08-04
EP3184112A1 (en) 2017-06-28
TW201416357A (zh) 2014-05-01
RU2015108790A (ru) 2016-10-10
KR20170001723A (ko) 2017-01-04
CY1121617T1 (el) 2020-07-31
PT2883866T (pt) 2019-04-05
CA2880794A1 (en) 2014-02-20
KR20170001722A (ko) 2017-01-04
US9221865B2 (en) 2015-12-29
HRP20190572T1 (hr) 2019-05-17
EP2883866B1 (en) 2019-02-27
LT2883866T (lt) 2019-05-10
EP3184112B1 (en) 2020-12-23
WO2014027658A1 (ja) 2014-02-20
DK2883866T3 (da) 2019-05-13
AU2013303534A1 (en) 2015-02-26
EP2883866A1 (en) 2015-06-17
ES2718307T3 (es) 2019-07-01
CN104540803A (zh) 2015-04-22
TWI603966B (zh) 2017-11-01
CN104540803B (zh) 2018-04-24
US9475835B2 (en) 2016-10-25
BR112015003041B1 (pt) 2022-07-26
HK1208436A1 (en) 2016-03-04
MX2015001935A (es) 2015-06-22
AU2013303534B2 (en) 2016-06-30
JP2016185979A (ja) 2016-10-27
US20160362389A1 (en) 2016-12-15
US10093645B2 (en) 2018-10-09
PL2883866T3 (pl) 2019-07-31
JPWO2014027658A1 (ja) 2016-07-28
HUE044412T2 (hu) 2019-10-28
US20160024132A1 (en) 2016-01-28
EP2883866A4 (en) 2016-06-15
US20180327377A1 (en) 2018-11-15
RS58568B1 (sr) 2019-05-31
CA2880794C (en) 2018-08-28
JP6518214B2 (ja) 2019-05-22
KR101770248B1 (ko) 2017-08-22
CN107011168B (zh) 2020-06-09
KR102010804B1 (ko) 2019-08-14
RU2633355C2 (ru) 2017-10-12
IL237086B (en) 2021-02-28
IL237086A0 (en) 2015-03-31

Similar Documents

Publication Publication Date Title
BR112015003041A2 (pt) Intermediário para síntese de 1-(2-desóxi-2-fluoro-4 -tio-\beta-d-arabinofuranosil)citosina , intermediário para síntese de tionucleosídeo , e métodos para produzir estes intermediários
CO7061071A2 (es) Procesos para la preparación de (s)-1-(3-etoxi-4-metoxifenil)-2-metansulfoniletilamina
EP2951139A4 (en) SYNTHESIS FROM 1,1,2,3-TETRACHLORPROPENE
DK2895101T3 (da) Forbedret kirurgisk template
FI20126341A (fi) Menetelmä mikrofibrilloidun selluloosan valmistamiseksi, josta vesi on poistettu
EP2935168A4 (en) SYNTHESIS OF 3,3,3-TRIFLUOROPROPYNE
FI20125875A (fi) Jarru
UY34380A (es) ?determinación de polimorfismos de nucleótido simple útiles para predecir la respuesta clínica al acetato de glatirámero?.
BR112015002464A2 (pt) processo para a preparação de carbamat-benzoxazinonas, carbamat-benzoxazinonas e utilização das carbamat-benzoxazinonas
DK2885136T3 (da) Planteproducerende skriveinstrument
FR2959228B1 (fr) Nucleotides modifies
FI20126292A (fi) Menetelmä glassiinipaperin valmistamiseksi
BR112012025490A2 (pt) ''método para produção de 1,5 oebtanodiamina''
TWI561253B (en) Arctigenin derivative-containing antiager
DK2914574T3 (da) Ny fremgangsmåde
ITTO20110857A1 (it) Procedimento per la produzione di cicloesanonossina.
IT1397233B1 (it) Procedimento migliorativo per la sintesi del mono-acetil ganciclovir, intermedio chiave per la sintesi del valganciclovir.
DE112011104543A5 (de) Kopfbedeckung
GB201219906D0 (en) Matrix binders, uses & methods of manufacture
ES1077521Y (es) Percha para cascos
ES1076942Y (es) Pedal para instrumentos de percusión
IT1404226B1 (it) Procedimento per la produzione di fibrocemento ecologico, fibrocemento ottenuto e suoi impieghi.
FI9783U1 (fi) Akustinen kielisoitin
CO6910041A1 (es) Procedimiento para la fabricacion de ataudes ecologicos
BR302012005614S1 (pt) "configuração aplicada em arandela"

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 13/08/2013, OBSERVADAS AS CONDICOES LEGAIS

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: REF. RPI 2690 DE 26/07/2022 QUANTO AO TITULO.