AR029181A1 - Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter - Google Patents

Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter

Info

Publication number
AR029181A1
AR029181A1 ARP000105064A ARP000105064A AR029181A1 AR 029181 A1 AR029181 A1 AR 029181A1 AR P000105064 A ARP000105064 A AR P000105064A AR P000105064 A ARP000105064 A AR P000105064A AR 029181 A1 AR029181 A1 AR 029181A1
Authority
AR
Argentina
Prior art keywords
rapamycin
ether
silil
eter
intermediate compound
Prior art date
Application number
ARP000105064A
Other languages
English (en)
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of AR029181A1 publication Critical patent/AR029181A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un procedimiento regioselectivo para la preparacion de un éster o éter de rapamicina en posicion 42 que tiene la estructura segun formula (1), en la cual R es un éster o éter, caracterizado porque comprende: (a) tratar rapamicina con agente sililante para formar 31,42-bis silil éter de rapamicina; (b) hidrolizar selectivamente el 42-silil éter en ácido liviano para proveer 31-silil éter de rapamicina; (c) tratar el 31-silil éter de rapamicina con un reactivo apropiado esterificante o eterificante para formar 31-silil éter 42-éster o éter de rapamicina; y (d) hidrolizar selectivamente el 31-silil éter en ácido liviano para proveer el 42-éster o éter de rapamicina deseado.
ARP000105064A 1999-09-29 2000-09-27 Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter AR029181A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US40883099A 1999-09-29 1999-09-29

Publications (1)

Publication Number Publication Date
AR029181A1 true AR029181A1 (es) 2003-06-18

Family

ID=23617953

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000105064A AR029181A1 (es) 1999-09-29 2000-09-27 Procedimiento regioselectivo de derivados de rapamicina y compuestos intermediarios de 31-silil eter

Country Status (24)

Country Link
EP (1) EP1216251B1 (es)
JP (1) JP4289813B2 (es)
KR (1) KR100754236B1 (es)
CN (1) CN1176925C (es)
AR (1) AR029181A1 (es)
AT (1) ATE233269T1 (es)
AU (1) AU782234B2 (es)
BR (1) BR0014433A (es)
CA (1) CA2385461C (es)
CZ (1) CZ300368B6 (es)
DE (1) DE60001510T2 (es)
DK (1) DK1216251T3 (es)
EA (1) EA004331B1 (es)
ES (1) ES2189768T3 (es)
HK (1) HK1044774B (es)
HU (1) HUP0202609A3 (es)
IL (2) IL148542A0 (es)
MX (1) MXPA02003243A (es)
NO (1) NO20021360L (es)
NZ (1) NZ517644A (es)
PL (1) PL200899B1 (es)
TW (1) TWI256395B (es)
WO (1) WO2001023395A2 (es)
ZA (1) ZA200201918B (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
SG145716A1 (en) 2003-09-03 2008-09-29 Wyeth Corp Amorphous rapamycin 42-ester with 3-hydroxy-2- (hydroxymethyl)-2- methylpropionic acid and pharmaceutical compositions containing the same
AR046194A1 (es) 2003-11-04 2005-11-30 Mayo Foundation Metodo de tratamiento del linfoma de celulas del manto
AU2005238431A1 (en) * 2004-04-14 2005-11-10 Wyeth Regiospecific synthesis of rapamycin 42-ester derivatives
AU2005233612A1 (en) 2004-04-14 2005-10-27 Wyeth Proline CCI-779 (proline-rapamycin 42-ester with 2,2-bis (hydroxymethyl) propionic acid) and two-step enzymatic synthesis of proline CCI-779 and CCI-779 using microbial lipase
JP2008517874A (ja) 2004-08-10 2008-05-29 ワイス Ｃｃｉ−７７９誘導体及びそれらの作製法
CN102886045A (zh) 2005-02-03 2013-01-23 综合医院公司 治疗吉非替尼耐药性癌症的方法
CA2595766A1 (en) 2005-02-09 2006-08-17 Wyeth Cci-779 polymorph and use thereof
EP1942937A1 (en) 2005-11-04 2008-07-16 Wyeth Antineoplastic combinations with mtor inhibitor, herceptin, and/or hki-272
US8022216B2 (en) 2007-10-17 2011-09-20 Wyeth Llc Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof
PL2310011T3 (pl) 2008-06-17 2013-12-31 Wyeth Llc Kombinacje przeciwnowotworowe zawierające HKI-272 i vinorelbine
CN101676291B (zh) 2008-09-18 2012-05-09 上海海和药物研究开发有限公司 一类雷帕霉素碳酸酯类似物、其药物组合物及其制备方法和用途
AU2011210227A1 (en) * 2010-01-28 2012-08-30 Fresenius Kabi Oncology Ltd. Process for the preparation of Temsirolimus and its intermediates
CN102020662B (zh) 2011-01-07 2013-02-13 天津市炜杰科技有限公司 一种驮瑞塞尔制备方法
BR112013025085A2 (pt) * 2011-04-01 2016-07-19 Sandoz Ag processo para a acilação de rapamicina e processo para sintetizar tensirolimo
CN103421023B (zh) * 2013-07-30 2015-09-23 福建省微生物研究所 一种替西罗莫司的合成工艺
CN104086564B (zh) * 2014-07-30 2019-02-05 江苏奥赛康药业股份有限公司 一种高纯度坦罗莫司的制备方法
CN106146536B (zh) * 2015-04-25 2019-07-26 山东新时代药业有限公司 一种依维莫司的制备方法
WO2017158499A1 (en) * 2016-03-14 2017-09-21 Wisconsin Alumni Research Foundation Oligolactic acid conjugates and micelles with enhanced anticancer efficacy
CN107561170B (zh) * 2016-07-02 2021-07-30 山东新时代药业有限公司 一种坦西莫司中间体的分析检测方法
CN108948045A (zh) * 2017-05-20 2018-12-07 鲁南制药集团股份有限公司 一种替西罗莫司的制备方法
CN108948046B (zh) * 2017-05-20 2020-11-10 鲁南制药集团股份有限公司 一种替西罗莫司的中间体及其制备方法
CN109206441B (zh) * 2017-06-30 2022-05-20 正大天晴药业集团股份有限公司 一种依维莫司的纯化方法
CN109776570A (zh) * 2017-11-14 2019-05-21 上海医药工业研究院 一种依维莫司中间体、其制备方法及其应用
SG11202012447YA (en) 2018-06-15 2021-01-28 Navitor Pharm Inc Rapamycin analogs and uses thereof
CN109369679A (zh) * 2018-12-24 2019-02-22 江苏卓和药业有限公司 一种雷帕霉素的精制方法
CN109851626B (zh) * 2019-01-08 2021-11-02 扬子江药业集团四川海蓉药业有限公司 一种替西罗莫司的分离纯化方法
TW202134234A (zh) 2019-12-05 2021-09-16 美商奈維特製藥公司 雷帕黴素類似物及其用途
CN113372359A (zh) * 2020-03-10 2021-09-10 鲁南制药集团股份有限公司 一种坦西莫司的制备方法
CN114106014B (zh) * 2020-08-27 2024-03-15 鲁南制药集团股份有限公司 一种依维莫司的制备方法
CN115028658A (zh) * 2022-07-06 2022-09-09 国药集团川抗制药有限公司 雷帕霉素硅醇酯及其制备方法和应用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5120842A (en) * 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5387680A (en) * 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5362718A (en) * 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5563145A (en) * 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines

Also Published As

Publication number Publication date
IL148542A0 (en) 2002-09-12
ZA200201918B (en) 2003-08-27
PL354461A1 (en) 2004-01-12
HK1044774B (zh) 2003-05-30
KR100754236B1 (ko) 2007-09-03
CZ20021136A3 (cs) 2002-06-12
TWI256395B (en) 2006-06-11
WO2001023395A2 (en) 2001-04-05
IL148542A (en) 2006-08-20
WO2001023395A3 (en) 2001-10-25
HUP0202609A3 (en) 2004-11-29
ES2189768T3 (es) 2003-07-16
EA004331B1 (ru) 2004-04-29
ATE233269T1 (de) 2003-03-15
CA2385461A1 (en) 2001-04-05
JP2003510329A (ja) 2003-03-18
DE60001510T2 (de) 2003-10-02
CZ300368B6 (cs) 2009-05-06
PL200899B1 (pl) 2009-02-27
KR20020029796A (ko) 2002-04-19
CA2385461C (en) 2009-03-17
HUP0202609A2 (hu) 2002-12-28
EA200200412A1 (ru) 2002-10-31
JP4289813B2 (ja) 2009-07-01
EP1216251B1 (en) 2003-02-26
HK1044774A1 (en) 2002-11-01
DK1216251T3 (da) 2003-06-16
CN1402731A (zh) 2003-03-12
EP1216251A2 (en) 2002-06-26
AU7718200A (en) 2001-04-30
NO20021360D0 (no) 2002-03-19
NO20021360L (no) 2002-03-19
DE60001510D1 (de) 2003-04-03
MXPA02003243A (es) 2002-09-30
AU782234B2 (en) 2005-07-14
NZ517644A (en) 2003-09-26
CN1176925C (zh) 2004-11-24
BR0014433A (pt) 2002-06-11

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