ES2130542T3 - 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-ona.

Info

Publication number
ES2130542T3
ES2130542T3 ES95308030T ES95308030T ES2130542T3 ES 2130542 T3 ES2130542 T3 ES 2130542T3 ES 95308030 T ES95308030 T ES 95308030T ES 95308030 T ES95308030 T ES 95308030T ES 2130542 T3 ES2130542 T3 ES 2130542T3
Authority
ES
Spain
Prior art keywords
ona
difluoro
preparing
ribofuranosil
desoxi
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES95308030T
Other languages
English (en)
Inventor
Richard Alan Berglund
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=23397211&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2130542(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2130542T3 publication Critical patent/ES2130542T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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

LA INVENCION SUMINISTRA UN PROCESO PARA PREPARAR HIDROCLORURO DE GEMCITABINA QUE COMPRENDE EL DESBLOQUEO DE {BE}-1-(2''-DEOXI2'',2''-DIFLUORO-3'',5''-DI-O-BENZOILO-D-RIBO-FURANOSIL)-4AMINOPIRIMIDINA-2-ONA CON UNA CANTIDAD CATALITIDA DE UN ALQUILAMINO EN LA PRESENCIA DE METANOL O ETANOL EN UN AMBIENTE ESENCIALMENTE LIBRE DE AGUA; EL TRATAMIENTO DE LA SOLUCION RESULTANTE CON ACIDO HIDROCLORICO Y UN ANTISOLVENTE; Y LA RECUPERACION DEL HIDROCLORURO DE GEMCITABINA SOLIDO, RESULTANTE.
ES95308030T 1994-12-13 1995-11-09 Procedimiento para preparar clorhidrato de 1-(2'-desoxi-2',2'-difluoro-d-ribofuranosil)-4-aminopirimidin-2-ona. Expired - Lifetime ES2130542T3 (es)

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
ES2130542T3 true ES2130542T3 (es) 1999-07-01

Family

ID=23397211

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95308030T Expired - Lifetime ES2130542T3 (es) 1994-12-13 1995-11-09 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 (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
PE20000042A1 (es) * 1997-12-22 2000-02-17 Schering Corp Uso combinado de un inhibidor de farnesilo transferasa y un agente antineoplasico y/o terapia de radiacion para el tratamiento de enfermedades proliferativas
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
WO2006015346A1 (en) * 2004-07-30 2006-02-09 Pharmaessentia Corp. STEREOSELECTIVE SYNTHESIS OF β-NUCLEOSIDES
WO2006070985A1 (en) * 2004-12-30 2006-07-06 Hanmi Pharm. Co., Ltd. METHOD FOR THE PREPARATION OF 2#-DEOXY-2#,2#-DIFLUOROCYTIDINE
JP2008531680A (ja) * 2005-03-04 2008-08-14 ダブール・ファーマ・リミテッド βアノマーが富化された２１−デオキシ−２１，２１−ジフルオロ−Ｄ−リボフラノシルヌクレオシドの調製のための中間体と方法
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
TWI368621B (en) * 2005-05-02 2012-07-21 Leyoung Biotech Co Ltd 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
JP2009513623A (ja) 2005-10-28 2009-04-02 アーチ ファーマラブズ リミテッド 塩酸ジェムシタビンの改良された製造方法
KR101259637B1 (ko) * 2005-12-14 2013-04-30 주식회사종근당 1-(2´-데옥시-2´,2´-디플루오로-디-리보푸라노실)-4-아미노피리미딘-2-온또는 그의 염산염의 제조방법
RU2345087C2 (ru) * 2006-02-06 2009-01-27 Др. Редди`С Лабораторис Лтд. Способ получения и очистки гемцитабина гидрохлорида
US8912321B2 (en) * 2006-10-10 2014-12-16 Gilead Pharmasset Llc Preparation of nucleosides ribofuranosyl pyrimidines
US20090069354A1 (en) * 2007-09-12 2009-03-12 Protia, Llc Deuterium-enriched gemcitabine
JO2778B1 (en) 2007-10-16 2014-03-15 ايساي انك Certain Compounds, Compositions and Methods
TWI415858B (zh) * 2007-11-06 2013-11-21 Pharmaessentia Corp β－核苷之新穎合成技術
IT1393062B1 (it) * 2008-10-23 2012-04-11 Prime Europ Therapeuticals Procedimento per la preparazione di gemcitabina cloridrato
US8609631B2 (en) 2009-04-06 2013-12-17 Eisai Inc. Compositions and methods for treating cancer
AU2010234562B2 (en) * 2009-04-06 2016-05-12 Taiho Pharmaceutical Co., Ltd. Combination of cytidine-based antineoplastic drugs with cytidine deaminase inhibitor and use thereof in the treatment of cancer
JP5687687B2 (ja) * 2009-04-06 2015-03-18 大塚製薬株式会社 癌を治療するための（２’−デオキシ−リボフラノシル）−１，３，４，７−テトラヒドロ−（１，３）ジアゼピン−２−オン誘導体
UY32546A (es) * 2009-04-06 2010-10-29 Eisai Inc Composiciones y metodos para tratar 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
EP2431376B2 (en) * 2009-05-15 2024-02-07 Delta-Fly Pharma, Inc. Novel stable crystal of 1-(2'-cyano-2'-deoxy-beta -d-arabinofuranosyl)cytosine monohydrochloride
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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE92499T1 (de) * 1984-12-04 1993-08-15 Lilly Co Eli Tumorbehandlung bei saeugetieren.
US4965374A (en) * 1987-08-28 1990-10-23 Eli Lilly And Company Process for and intermediates of 2',2'-difluoronucleosides
US5223608A (en) * 1987-08-28 1993-06-29 Eli Lilly And Company Process for and intermediates of 2',2'-difluoronucleosides
JPH0673086A (ja) * 1992-06-22 1994-03-15 Eli Lilly & Co 立体選択的な陰イオングリコシル化法
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
UA41261C2 (uk) * 1992-06-22 2001-09-17 Елі Ліллі Енд Компані Спосіб одержання збагачених бета-аномером нуклеозидів
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

Also Published As

Publication number Publication date
DE69509624D1 (de) 1999-06-17
IL115852A0 (en) 1996-01-31
HUT77929A (hu) 1998-11-30
GR3030265T3 (en) 1999-08-31
MX9704322A (es) 1997-09-30
UA48152C2 (uk) 2002-08-15
IL115852A (en) 1999-09-22
YU49314B (sh) 2005-06-10
US5808048A (en) 1998-09-15
EP0719788A3 (en) 1996-09-25
CZ179897A3 (en) 1997-09-17
WO1996018637A1 (en) 1996-06-20
NZ296476A (en) 1998-12-23
NO306783B1 (no) 1999-12-20
KR100424991B1 (ko) 2004-05-20
TW379226B (en) 2000-01-11
NO972679D0 (no) 1997-06-11
EP0719788B1 (en) 1999-05-12
RU2154648C2 (ru) 2000-08-20
HU219021B (hu) 2001-01-29
PL321046A1 (en) 1997-11-24
DE69509624T2 (de) 1999-10-07
NO972679L (no) 1997-06-11
AU689674B2 (en) 1998-04-02
PE49296A1 (es) 1996-11-21
DK0719788T3 (da) 1999-11-01
US5637688A (en) 1997-06-10
AU4110196A (en) 1996-07-03
BR9509979A (pt) 1998-06-09
AR001041A1 (es) 1997-09-24
ZA959320B (en) 1997-05-05
MY112488A (en) 2001-06-30
BG101591A (en) 1998-03-31
ATE179986T1 (de) 1999-05-15
BG62738B1 (bg) 2000-06-30
CO4520286A1 (es) 1997-10-15
CZ290941B6 (cs) 2002-11-13
EP0719788A2 (en) 1996-07-03
SI0719788T1 (en) 1999-10-31
YU70895A (sh) 1998-09-18
RO117327B1 (ro) 2002-01-30
PL181732B1 (en) 2001-09-28
JPH10510806A (ja) 1998-10-20
CN1047177C (zh) 1999-12-08
CN1169728A (zh) 1998-01-07

Similar Documents

Publication Publication Date Title
ES2130542T3 (es) Procedimiento para preparar clorhidrato de 1-(2'-desoxi-2',2'-difluoro-d-ribofuranosil)-4-aminopirimidin-2-ona.
LU93229I2 (fr) "pitolisant et ses sels pharmaceutiquement acceptables, tel que chlorhydrate"
CO5011096A1 (es) Medicamentos que contienen antagonistas del receptor 5-ht3 para el tratamiento de la ibs
BR9813508A (pt) Inibição de replicação viral associada com membrana
BRPI0109198B8 (pt) emplastro tendo um apoio
AU4470097A (en) Pharmaceutical preparations comprised of salts of hyaluronic acid with local anaesthetics
ATE177657T1 (de) Intravaginales wirkstoffabgabesystem
ES2093735T3 (es) Derivados de melatonina para uso en la terapia de trastornos del sueño y en medicacion preanestesica.
NO174801C (es)
ES2192779T3 (es) Modificacion cristalina de 1-(2,6-difluorbencil)-1h-1,2,3-triazol-4-carboxamida y su uso como antiepileptico.
BRPI0012553B8 (pt) pastilha contendo cloridrato de ambroxol, seu processo de preparação e seu uso
TR200000697T2 (tr) İkame edilmiş 1,2,3,4,5,6-Heksahidro-2,6-Metano-3-Benzazosin-10-OL'ler, üretim yöntemleri ve farmasötik preparat olarak kullanımları.
FI963394A0 (fi) Yskää vastustava koostumus, joka sisältää yskää vastustavaa ainetta ja bentsydamiinia
BR9814188A (pt) "agonistas de 5-ht1f"
BR9910185A (pt) Uso de um composto, e, processo para o tratamento de um paciente que sofre de, ou em risco de, uma doença micobacteriana
ES8403463A1 (es) "un procedimiento para la preparacion de un compuesto de imidazol".
GB0004708D0 (en) Restricting reinstatement of drug use
ATE100451T1 (de) Substituierte bisazole, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel.
SE9802538D0 (sv) New pharmaceutically active compounds
TR199901958T2 (xx) �nfertiliteye kar�� ve fertiliteyi art�rmak i�in bir ila�.
IL89401A0 (en) Medicaments containing 1,4-dihydropyridine derivatives for the treatment of alcohol addiction
WO1998052548A3 (de) Verwendung von 1-ar(alk)yl-imidazolin-2-one zur behandlung von angst- und spannungszuständen
ECSP951607A (es) Procedimiento para preparar clorhidrato de 1-(2' - desoxi - 2', 2'- difluoro - d - ribofuranosil) - 4 - aminopirimidin - 2 - ona, case x - 8961
ES2146200T3 (es) Medicamentos inducidos peritonealmente.
ITMI20001041A0 (it) Procedimento atto all'esercizio di un sistema di alimentazione del carburante.

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 719788

Country of ref document: ES