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 eterInfo
- 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
Links
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 title 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 8
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 abstract 7
- 229960002930 sirolimus Drugs 0.000 abstract 7
- 239000002253 acid Substances 0.000 abstract 2
- 150000002148 esters Chemical class 0.000 abstract 2
- 230000003301 hydrolyzing effect Effects 0.000 abstract 2
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
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.
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)
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)
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 |
-
2000
- 2000-09-14 TW TW089118799A patent/TWI256395B/zh active
- 2000-09-27 AR ARP000105064A patent/AR029181A1/es unknown
- 2000-09-27 KR KR1020027004033A patent/KR100754236B1/ko not_active IP Right Cessation
- 2000-09-27 EA EA200200412A patent/EA004331B1/ru not_active IP Right Cessation
- 2000-09-27 CA CA002385461A patent/CA2385461C/en not_active Expired - Fee Related
- 2000-09-27 CN CNB008163685A patent/CN1176925C/zh not_active Expired - Fee Related
- 2000-09-27 JP JP2001526545A patent/JP4289813B2/ja not_active Expired - Fee Related
- 2000-09-27 NZ NZ517644A patent/NZ517644A/en unknown
- 2000-09-27 IL IL14854200A patent/IL148542A0/xx active IP Right Grant
- 2000-09-27 DE DE60001510T patent/DE60001510T2/de not_active Expired - Lifetime
- 2000-09-27 PL PL354461A patent/PL200899B1/pl not_active IP Right Cessation
- 2000-09-27 HU HU0202609A patent/HUP0202609A3/hu unknown
- 2000-09-27 WO PCT/US2000/026445 patent/WO2001023395A2/en active IP Right Grant
- 2000-09-27 ES ES00966904T patent/ES2189768T3/es not_active Expired - Lifetime
- 2000-09-27 MX MXPA02003243A patent/MXPA02003243A/es active IP Right Grant
- 2000-09-27 AT AT00966904T patent/ATE233269T1/de not_active IP Right Cessation
- 2000-09-27 BR BR0014433-9A patent/BR0014433A/pt not_active IP Right Cessation
- 2000-09-27 AU AU77182/00A patent/AU782234B2/en not_active Ceased
- 2000-09-27 CZ CZ20021136A patent/CZ300368B6/cs not_active IP Right Cessation
- 2000-09-27 DK DK00966904T patent/DK1216251T3/da active
- 2000-09-27 EP EP00966904A patent/EP1216251B1/en not_active Expired - Lifetime
-
2002
- 2002-03-06 IL IL148542A patent/IL148542A/en not_active IP Right Cessation
- 2002-03-07 ZA ZA200201918A patent/ZA200201918B/en unknown
- 2002-03-19 NO NO20021360A patent/NO20021360L/no not_active Application Discontinuation
- 2002-09-02 HK HK02106469.7A patent/HK1044774B/zh not_active IP Right Cessation
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Legal Events
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