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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (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) NO20021360D0 (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
RU2345999C2 (ru) * 2003-09-03 2009-02-10 Уайт Аморфный 42-эфир рапамицина и 3-гидрокси-2(гидроксиметил)-2-метилпропионовой кислоты и содержащие его фармацевтические композиции
AR046194A1 (es) 2003-11-04 2005-11-30 Mayo Foundation Metodo de tratamiento del linfoma de celulas del manto
BRPI0509854A (pt) 2004-04-14 2007-10-23 Wyeth Corp composto, métodos para a preparação regio-especìfica de um 42-éster de rapamicina ou 42-éster de prolina-rapamicina e para a preparação de um 42-éster de prolina-rapamicina, composição, e, produto
US7268144B2 (en) * 2004-04-14 2007-09-11 Wyeth Regiospecific synthesis of rapamycin 42-ester derivatives
MX2007001676A (es) 2004-08-10 2007-04-12 Wyeth Corp Derivados de 42-ester de rapamicina con acido 2,2-bis(hidroximetil)propionico y metodos para hacer los mismos.
NZ556673A (en) 2005-02-03 2010-03-26 Gen Hospital Corp Method for treating gefitinib and/or erlotinib resistant cancer with an EGFR inhibitor
JP2008530090A (ja) 2005-02-09 2008-08-07 ワイス Ｃｃｉ−７７９多形及びその使用
KR101354828B1 (ko) 2005-11-04 2014-02-18 와이어쓰 엘엘씨 ｍＴＯＲ 저해자, 헤르셉틴, 및/또는 ＨＫＩ-272의항신생물성 조합
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
EP3730139B1 (en) 2008-06-17 2023-08-16 Wyeth LLC Antineoplastic combinations containing hki-272 and 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
EP2528906A2 (en) * 2010-01-28 2012-12-05 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
RU2603261C2 (ru) * 2011-04-01 2016-11-27 Сандоз Аг Региоселективное ацилирование рапамицина в положении с-42
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
KR102420468B1 (ko) * 2016-03-14 2022-07-13 위스콘신 얼럼나이 리서어치 화운데이션 올리고락트산 컨쥬게이트 및 향상된 항암 효능을 갖는 마이셀
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
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
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
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
DK3813946T3 (da) 2018-06-15 2024-08-19 Janssen Pharmaceutica Nv Rapamycin-analoger og anvendelser deraf
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
JP2023506410A (ja) 2019-12-05 2023-02-16 アナクリア セラピューティクス， インコーポレイテッド ラパマイシン類似体及びその使用
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
NZ517644A (en) 2003-09-26
EA200200412A1 (ru) 2002-10-31
CZ300368B6 (cs) 2009-05-06
BR0014433A (pt) 2002-06-11
KR100754236B1 (ko) 2007-09-03
DK1216251T3 (da) 2003-06-16
CN1176925C (zh) 2004-11-24
TWI256395B (en) 2006-06-11
WO2001023395A3 (en) 2001-10-25
ES2189768T3 (es) 2003-07-16
EP1216251A2 (en) 2002-06-26
JP2003510329A (ja) 2003-03-18
DE60001510T2 (de) 2003-10-02
CA2385461A1 (en) 2001-04-05
NO20021360L (no) 2002-03-19
PL354461A1 (en) 2004-01-12
KR20020029796A (ko) 2002-04-19
IL148542A (en) 2006-08-20
EP1216251B1 (en) 2003-02-26
EA004331B1 (ru) 2004-04-29
HUP0202609A3 (en) 2004-11-29
CN1402731A (zh) 2003-03-12
PL200899B1 (pl) 2009-02-27
AU782234B2 (en) 2005-07-14
IL148542A0 (en) 2002-09-12
ATE233269T1 (de) 2003-03-15
JP4289813B2 (ja) 2009-07-01
CZ20021136A3 (cs) 2002-06-12
HK1044774A1 (en) 2002-11-01
ZA200201918B (en) 2003-08-27
HK1044774B (zh) 2003-05-30
HUP0202609A2 (hu) 2002-12-28
DE60001510D1 (de) 2003-04-03
NO20021360D0 (no) 2002-03-19
MXPA02003243A (es) 2002-09-30
CA2385461C (en) 2009-03-17
AU7718200A (en) 2001-04-30
WO2001023395A2 (en) 2001-04-05

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