AR001041A1 - Procedimiento para preparar clorhidrato de 1-(2'-desoxi-2'2'-difluoro-d-ribofuranosil)-4-aminopirimidin-2-ona - Google Patents
Procedimiento para preparar clorhidrato de 1-(2'-desoxi-2'2'-difluoro-d-ribofuranosil)-4-aminopirimidin-2-onaInfo
- Publication number
- AR001041A1 AR001041A1 AR33407495A AR33407495A AR001041A1 AR 001041 A1 AR001041 A1 AR 001041A1 AR 33407495 A AR33407495 A AR 33407495A AR 33407495 A AR33407495 A AR 33407495A AR 001041 A1 AR001041 A1 AR 001041A1
- Authority
- AR
- Argentina
- Prior art keywords
- ribofuranosyl
- deoxy
- difluoro
- hydrochloride
- prepare
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Saccharide Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Se proporciona un procedimiento para preparar clorhidrato de 1-(2-desoxi-2,2-difluoro-D-ribofuranosil)-4-aminopiridin-2-ona clorhidratode gemcitabina de fórmula (I), separando los grupos benzoilo de bloqueo de compuestos debeta-1-(2-desoxi-2,2-difluoro-3,5-di-O-benzoil-D-ribofuranosil)-4- aminopirimidina-2-ona en presencia de cantidades catalíticas de alquilaminas,enun medio solvente de metanol o etanol, bajo exclusión de agua. El clorhidrato gemcitabina se recuperatratando la solución formada con ácido clorhídrico y unantisolvente.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/355,372 US5637688A (en) | 1994-12-13 | 1994-12-13 | Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride |
Publications (1)
Publication Number | Publication Date |
---|---|
AR001041A1 true AR001041A1 (es) | 1997-09-24 |
Family
ID=23397211
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR33407495A AR001041A1 (es) | 1994-12-13 | 1995-11-01 | Procedimiento para preparar clorhidrato de 1-(2'-desoxi-2'2'-difluoro-d-ribofuranosil)-4-aminopirimidin-2-ona |
Country Status (31)
Country | Link |
---|---|
US (2) | US5637688A (es) |
EP (1) | EP0719788B1 (es) |
JP (1) | JPH10510806A (es) |
KR (1) | KR100424991B1 (es) |
CN (1) | CN1047177C (es) |
AR (1) | AR001041A1 (es) |
AT (1) | ATE179986T1 (es) |
AU (1) | AU689674B2 (es) |
BG (1) | BG62738B1 (es) |
BR (1) | BR9509979A (es) |
CO (1) | CO4520286A1 (es) |
CZ (1) | CZ290941B6 (es) |
DE (1) | DE69509624T2 (es) |
DK (1) | DK0719788T3 (es) |
ES (1) | ES2130542T3 (es) |
GR (1) | GR3030265T3 (es) |
HU (1) | HU219021B (es) |
IL (1) | IL115852A (es) |
MY (1) | MY112488A (es) |
NO (1) | NO306783B1 (es) |
NZ (1) | NZ296476A (es) |
PE (1) | PE49296A1 (es) |
PL (1) | PL181732B1 (es) |
RO (1) | RO117327B1 (es) |
RU (1) | RU2154648C2 (es) |
SI (1) | SI0719788T1 (es) |
TW (1) | TW379226B (es) |
UA (1) | UA48152C2 (es) |
WO (1) | WO1996018637A1 (es) |
YU (1) | YU49314B (es) |
ZA (1) | ZA959320B (es) |
Families Citing this family (30)
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US5637688A (en) * | 1994-12-13 | 1997-06-10 | Eli Lilly And Company | Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride |
EP0870506A1 (en) * | 1997-04-11 | 1998-10-14 | Eli Lilly And Company | Compositions comprising a cryptophycin compound in combination with a synchronizing or activating agent for treating cancer |
TW581763B (en) * | 1997-12-22 | 2004-04-01 | Schering Corp | Combination and pharmaceutical composition comprising FPT inhibitor for treating proliferative diseases |
US6376470B1 (en) | 1999-09-23 | 2002-04-23 | Enzon, Inc. | Polymer conjugates of ara-C and ara-C derivatives |
WO2002028387A1 (en) * | 2000-10-03 | 2002-04-11 | Oncopharmaceutical, Inc. | Inhibitors of angiogenesis and tumor growth for local and systemic administration |
WO2005014010A1 (en) * | 2003-07-24 | 2005-02-17 | Eli Lilly And Company | Pharmaceutical composition comprising gemcitabine and cyclodextrines |
US7214791B2 (en) * | 2004-07-01 | 2007-05-08 | Shenzhen Hande Technology Co., Ltd. | Method for preparation of 2′-deoxy-2′, 2′-difluoro-β-cytidine or pharmaceutically acceptable salts thereof by using 1,6-anhydro-β-d-glucose as raw material |
EP1812457A1 (en) * | 2004-07-30 | 2007-08-01 | Pharmaessentia Corp. | STEREOSELECTIVE SYNTHESIS OF ß-NUCLEOSIDES |
WO2006070985A1 (en) * | 2004-12-30 | 2006-07-06 | Hanmi Pharm. Co., Ltd. | METHOD FOR THE PREPARATION OF 2#-DEOXY-2#,2#-DIFLUOROCYTIDINE |
KR20070112774A (ko) * | 2005-03-04 | 2007-11-27 | 다브르 파마 리미티드 | 베타―아노머가 많은21데옥시,21,21-디플루오로-d-리보푸라노실뉴클레오시드의 제조를 위한 중간체 및 제조 방법 |
WO2006095359A1 (en) * | 2005-03-10 | 2006-09-14 | Sms Pharmaceuticals Limited | Synthesis of 2-deoxy-2, 2-di fluoro-d-ribo furanose-3, 5 di(4-methy/4-nitro-chloro)benzoate and its conversion to gemcitabine hydrochloride thereof |
US7485716B2 (en) * | 2005-05-02 | 2009-02-03 | Pharmaessentia Corp. | Stereoselective synthesis of β-nucleosides |
CN100391966C (zh) * | 2005-06-17 | 2008-06-04 | 华东师范大学 | 一种2’-脱氧-2’,2’-二氟-胞苷合成的方法 |
EP1940859A1 (en) | 2005-10-28 | 2008-07-09 | Arch Pharmalabs Limited | An improved process for preparation of gemcitabine hydrochloride |
KR101259637B1 (ko) * | 2005-12-14 | 2013-04-30 | 주식회사종근당 | 1-(2´-데옥시-2´,2´-디플루오로-디-리보푸라노실)-4-아미노피리미딘-2-온또는 그의 염산염의 제조방법 |
US20090069354A1 (en) * | 2007-09-12 | 2009-03-12 | Protia, Llc | Deuterium-enriched gemcitabine |
JO2778B1 (en) | 2007-10-16 | 2014-03-15 | ايساي انك | Certain vehicles, installations and methods |
CN101883570B (zh) * | 2007-11-06 | 2013-06-19 | 药华医药股份有限公司 | β-核苷的新颖合成 |
IT1393062B1 (it) * | 2008-10-23 | 2012-04-11 | Prime Europ Therapeuticals | Procedimento per la preparazione di gemcitabina cloridrato |
US8329666B2 (en) * | 2009-04-06 | 2012-12-11 | Eisai Inc. | Compositions and methods for treating cancer |
CA2757745C (en) * | 2009-04-06 | 2018-02-13 | Eisai Inc. | Combination of cytidine-based antineoplastic drugs with cytidine deaminase inhibitor and use thereof in the treatment of cancer |
US8609631B2 (en) | 2009-04-06 | 2013-12-17 | Eisai Inc. | Compositions and methods for treating cancer |
CA2757743C (en) * | 2009-04-06 | 2017-10-10 | Eisai Inc. | (2'-deoxy-ribofuranosyl)-1,3,4,7-tetrahydro-(1,3) diazepin-2-0ne derivatives for treating cancer |
CN101525361B (zh) * | 2009-04-21 | 2010-11-17 | 济南圣鲁金药物技术开发有限公司 | 基于吉西他滨结构的前药及其合成方法及应用 |
RU2538593C2 (ru) * | 2009-05-15 | 2015-01-10 | Дельта-Флай Фарма, Инк. | НОВЫЕ СТАБИЛЬНЫЕ КРИСТАЛЛЫ МОНОГИДРОХЛОРИДА 1-(2-β-D-АРАБИНОФУРАНОЗИЛ)ЦИТОЗИНА |
CN101628927B (zh) * | 2009-08-07 | 2012-10-10 | 卡硼瑞(北京)科技有限公司 | 以1,3,5-三-O-苯甲酰基-α-D-呋喃核糖为原料立体选择性制备β-二氟胞苷盐酸盐的方法 |
CN102453064B (zh) * | 2011-06-30 | 2014-07-09 | 江苏豪森药业股份有限公司 | 制备吉西他滨盐酸盐的方法 |
CN102659884B (zh) * | 2012-04-23 | 2014-07-02 | 南京臣功制药股份有限公司 | 盐酸吉西他滨的提纯方法 |
CN103224541B (zh) * | 2013-04-27 | 2015-07-01 | 江苏豪森药业股份有限公司 | 吉西他滨α-异构体转化回收工艺 |
CN104402945A (zh) * | 2014-11-27 | 2015-03-11 | 苏州乔纳森新材料科技有限公司 | 一种3-脱氧-1,2-o-异丙叉-d-呋喃木糖的合成方法 |
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US3817978A (en) * | 1971-06-16 | 1974-06-18 | Syntex Inc | 4-fluoro nucleosides and sugar intermediates, and methods of preparing |
JPS5924999B2 (ja) * | 1978-06-10 | 1984-06-13 | 富山化学工業株式会社 | 新規な5−フルオロ−2′−デオキシ−β−ウリジン誘導体の製造法 |
US4526988A (en) * | 1983-03-10 | 1985-07-02 | Eli Lilly And Company | Difluoro antivirals and intermediate therefor |
EP0184365B1 (en) * | 1984-12-04 | 1993-08-04 | Eli Lilly And Company | Improvements in the treatment of tumors in mammals |
US5223608A (en) * | 1987-08-28 | 1993-06-29 | Eli Lilly And Company | Process for and intermediates of 2',2'-difluoronucleosides |
US4965374A (en) * | 1987-08-28 | 1990-10-23 | Eli Lilly And Company | Process for and intermediates of 2',2'-difluoronucleosides |
UA41261C2 (uk) * | 1992-06-22 | 2001-09-17 | Елі Ліллі Енд Компані | Спосіб одержання збагачених бета-аномером нуклеозидів |
AU4134793A (en) * | 1992-06-22 | 1993-12-23 | Eli Lilly And Company | 2'-deoxy-2',2'-difluoro(2,6,8-substituted) purine nucleosides having anti-viral and anti-cancer activity and intermediates |
FI932871A (fi) * | 1992-06-22 | 1993-12-23 | Lilly Co Eli | Stereoselektiv anjonglykosylationsprocess |
KR100252451B1 (ko) * | 1992-09-01 | 2000-04-15 | 피터 지. 스트링거 | 뉴클레오사이드의아노머화방법 |
US5637688A (en) * | 1994-12-13 | 1997-06-10 | Eli Lilly And Company | Process for preparing 1-(2'-deoxy-2'-difluoro-d-ribofuranosyl)-4-aminopyrimidin-2-one hydrochloride |
-
1994
- 1994-12-13 US US08/355,372 patent/US5637688A/en not_active Expired - Lifetime
-
1995
- 1995-11-01 AR AR33407495A patent/AR001041A1/es unknown
- 1995-11-02 IL IL11585295A patent/IL115852A/xx not_active IP Right Cessation
- 1995-11-02 PE PE1995283631A patent/PE49296A1/es not_active IP Right Cessation
- 1995-11-03 ZA ZA959320A patent/ZA959320B/xx unknown
- 1995-11-09 DE DE69509624T patent/DE69509624T2/de not_active Expired - Lifetime
- 1995-11-09 SI SI9530272T patent/SI0719788T1/xx unknown
- 1995-11-09 ES ES95308030T patent/ES2130542T3/es not_active Expired - Lifetime
- 1995-11-09 AT AT95308030T patent/ATE179986T1/de active
- 1995-11-09 EP EP95308030A patent/EP0719788B1/en not_active Expired - Lifetime
- 1995-11-09 DK DK95308030T patent/DK0719788T3/da active
- 1995-11-10 CO CO95053319A patent/CO4520286A1/es unknown
- 1995-11-13 YU YU70895A patent/YU49314B/sh unknown
- 1995-11-14 TW TW084112041A patent/TW379226B/zh not_active IP Right Cessation
- 1995-11-14 JP JP8518835A patent/JPH10510806A/ja active Pending
- 1995-11-14 RU RU97111801/04A patent/RU2154648C2/ru not_active IP Right Cessation
- 1995-11-14 BR BR9509979A patent/BR9509979A/pt not_active Application Discontinuation
- 1995-11-14 RO RO97-01060A patent/RO117327B1/ro unknown
- 1995-11-14 CN CN95196792A patent/CN1047177C/zh not_active Expired - Fee Related
- 1995-11-14 PL PL95321046A patent/PL181732B1/pl unknown
- 1995-11-14 UA UA97062781A patent/UA48152C2/uk unknown
- 1995-11-14 WO PCT/US1995/014864 patent/WO1996018637A1/en active IP Right Grant
- 1995-11-14 KR KR1019970703880A patent/KR100424991B1/ko not_active IP Right Cessation
- 1995-11-14 CZ CZ19971798A patent/CZ290941B6/cs not_active IP Right Cessation
- 1995-11-14 HU HU9800673A patent/HU219021B/hu not_active IP Right Cessation
- 1995-11-14 NZ NZ296476A patent/NZ296476A/xx not_active IP Right Cessation
- 1995-11-14 AU AU41101/96A patent/AU689674B2/en not_active Ceased
- 1995-11-16 MY MYPI95003490A patent/MY112488A/en unknown
-
1997
- 1997-04-11 US US08/837,071 patent/US5808048A/en not_active Expired - Lifetime
- 1997-06-10 BG BG101591A patent/BG62738B1/bg unknown
- 1997-06-11 NO NO972679A patent/NO306783B1/no not_active IP Right Cessation
-
1999
- 1999-05-19 GR GR990401358T patent/GR3030265T3/el unknown
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