HUP0003954A2 - Eljárás és közbenső termékek pirrolo [2,3-d] pirimidin-származékok előállítására - Google Patents
Eljárás és közbenső termékek pirrolo [2,3-d] pirimidin-származékok előállításáraInfo
- Publication number
- HUP0003954A2 HUP0003954A2 HU0003954A HUP0003954A HUP0003954A2 HU P0003954 A2 HUP0003954 A2 HU P0003954A2 HU 0003954 A HU0003954 A HU 0003954A HU P0003954 A HUP0003954 A HU P0003954A HU P0003954 A2 HUP0003954 A2 HU P0003954A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- metal cation
- processes
- acid metal
- pyrimidine derivatives
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 239000000543 intermediate Substances 0.000 title abstract 2
- 150000004943 pyrrolo[2,3-d]pyrimidines Chemical class 0.000 title abstract 2
- 239000002184 metal Substances 0.000 abstract 4
- -1 cation salts Chemical class 0.000 abstract 3
- LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 150000001299 aldehydes Chemical class 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001768 cations Chemical class 0.000 abstract 1
- 229940014144 folate Drugs 0.000 abstract 1
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 abstract 1
- 235000019152 folic acid Nutrition 0.000 abstract 1
- 239000011724 folic acid Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
- C07C309/24—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of a carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/76—Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
-
- 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)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Cephalosporin Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
A jelen szabadalmi bejelentés tárgya (IV) általános képletű újszulfonsav fémkation sók, melyek folsav-gátló, 5-helyzetbenhelyettesített pirrolo[2,3-d]pirimidinek előállítása hasznos közbensőtermékkel. (IV) általános képletben: M jelentése fém kation; n értéke1, vagy 2; R2 jelentése NHCH(CO2R3)CH2CH2CO2R3, vagy OR3 képletűcsoport; R3 jelentése minden egyes előfordulásnál egymástólfüggetlenül karboxil védőcsoport; és X jelentése kötés; vagy 1-4szénatomos alkiléncsoport. A jelen találmány tárgya továbbá új eljárása szulfonsav fémkation sók előállítására, és új eljárás (III)általános képletű aldehidek előállítására a megfelelő szulfonsavfémkation sókból. A (III) általános képletben X és R2 jelentése afenti. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US93838597A | 1997-09-26 | 1997-09-26 | |
US9303997P | 1997-09-26 | 1997-09-26 | |
PCT/US1998/019560 WO1999016742A1 (en) | 1997-09-26 | 1998-09-18 | Processes and intermediates useful to make antifolates |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0003954A2 true HUP0003954A2 (hu) | 2001-09-28 |
HUP0003954A3 HUP0003954A3 (en) | 2002-12-28 |
Family
ID=26786718
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0003954A HUP0003954A3 (en) | 1997-09-26 | 1998-09-18 | Processes and intermediates useful to prepare pyrrolo [2,3-d] pyrimidine derivatives |
Country Status (18)
Country | Link |
---|---|
US (1) | US6013828A (hu) |
JP (1) | JP2001518459A (hu) |
KR (1) | KR20010030712A (hu) |
CN (2) | CN1213998C (hu) |
AU (1) | AU740087B2 (hu) |
BR (1) | BR9812524A (hu) |
CA (1) | CA2304656A1 (hu) |
CZ (1) | CZ301563B6 (hu) |
EA (1) | EA002452B3 (hu) |
HU (1) | HUP0003954A3 (hu) |
ID (1) | ID24165A (hu) |
IL (1) | IL135190A (hu) |
NO (2) | NO314456B1 (hu) |
NZ (1) | NZ503600A (hu) |
PL (1) | PL196216B1 (hu) |
TR (1) | TR200001220T2 (hu) |
UA (1) | UA53742C2 (hu) |
WO (1) | WO1999016742A1 (hu) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1212325A2 (en) * | 1999-08-23 | 2002-06-12 | Eli Lilly And Company | A novel crystalline form of disodium n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid salt and processes therefor |
PT1259513E (pt) * | 2000-02-25 | 2004-02-27 | Lilly Co Eli | Nova forma cristalina de acido n-¬4- ¬2-amino-4,7-dihidro -4-oxo-3h-pirrolo¬2,3-d|pirimidin-5-il)etil| - benzoil|-l-glutamico e processo para a sua obtencao |
CN100379729C (zh) * | 2006-04-06 | 2008-04-09 | 海南天源康泽医药科技有限公司 | 硝基化合物及其在培美曲塞制备中的应用 |
ES2354843T3 (es) * | 2006-08-14 | 2011-03-18 | Sicor, Inc. | Formas cristalinas de diácido de pemetrexed y procedimientos para la preparación de las mismas. |
KR20090052355A (ko) * | 2006-08-14 | 2009-05-25 | 시코르, 인크. | 순도가 높은 페메트렉세드 이산 및 이의 제조 방법 |
JP2010523589A (ja) * | 2007-04-03 | 2010-07-15 | ドクター レディズ ラボラトリーズ リミテッド | ペメトレキセドの固体形 |
CN101417998B (zh) | 2007-10-24 | 2012-10-24 | 重庆医药工业研究院有限责任公司 | 一种培美曲塞盐的纯化方法 |
CN101591247B (zh) * | 2008-05-30 | 2012-09-05 | 上海希迪制药有限公司 | 合成4-(4-甲酯基苯基)丁醛的方法 |
CN101684121B (zh) * | 2008-09-22 | 2013-04-03 | 重庆医药工业研究院有限责任公司 | 培美曲塞二酸的新晶型及其制备方法 |
US9174991B2 (en) | 2009-11-24 | 2015-11-03 | Azad Pharmaceutical Ingredients Ag | Crystalline form of pemetrexed disodium |
IT1401677B1 (it) * | 2010-07-22 | 2013-08-02 | Chemi Spa | Nuovo processo per la sintesi di pemetrexed sale disodico |
RU2552519C2 (ru) * | 2010-08-02 | 2015-06-10 | Неон Лэборэторис Лтд. | Способ получения высокочистого диалкилпеметрекседа |
WO2012111027A2 (en) * | 2011-02-15 | 2012-08-23 | Hetero Research Foundation | Process for pemetrexed disodium |
US9051322B2 (en) | 2011-03-23 | 2015-06-09 | Scinopharm Taiwan, Ltd. | Process for the production of a pemetrexed salt |
AU2011363636B2 (en) * | 2011-03-25 | 2016-03-17 | Scinopharm Taiwan Ltd | Process for the production of a pemetrexed salt |
WO2012150280A2 (en) | 2011-05-05 | 2012-11-08 | Lonza Ltd | Preparation of 4,4-dialkoxy-1-buten-1-ylarenes |
CN102911176B (zh) * | 2012-10-10 | 2015-07-22 | 德州德药制药有限公司 | 一种培美曲塞二钠的制备方法 |
CN102887902B (zh) * | 2012-10-10 | 2015-05-20 | 北京莱瑞森医药科技有限公司 | 一种合成高纯度培美酸的制备工艺 |
KR101578093B1 (ko) * | 2013-09-05 | 2015-12-16 | 주식회사 삼양바이오팜 | 고순도 페메트렉세드 제조를 위한 향상된 중간체 제조 방법 및 이를 사용하여 고순도 페메트렉세드를 제조하는 방법 |
NZ630292A (en) | 2013-11-25 | 2015-02-27 | Shilpa Medicare Ltd | Process for crystalline pemetrexed dipotassium salt |
CN104817563B (zh) * | 2015-05-11 | 2017-10-27 | 宁波美诺华药业股份有限公司 | 培美曲塞‑n,n‑二苄基乙二胺盐的制备方法 |
CN109836425B (zh) * | 2017-11-24 | 2023-01-24 | 江苏创诺制药有限公司 | 一种合成培美酸的制备工艺 |
CN109721604B (zh) * | 2019-01-25 | 2021-03-23 | 南京亚东启天药业有限公司 | 培美曲塞酸的制备方法 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4895946A (en) * | 1987-10-26 | 1990-01-23 | The Trustees Of Princeton University | Process for the preparation of fused pyridine compounds |
NO169490C (no) * | 1988-03-24 | 1992-07-01 | Takeda Chemical Industries Ltd | Analogifremgangsmaate for fremstilling av terapeutisk aktive pyrrolopyrimidinderivater |
JP2983254B2 (ja) * | 1989-06-14 | 1999-11-29 | 武田薬品工業株式会社 | ピロロ〔2,3―d〕ピリミジン誘導体の製造法およびその中間体 |
EP0438261A3 (en) * | 1990-01-16 | 1992-02-26 | Takeda Chemical Industries, Ltd. | Condensed heterocyclic glutamic acid derivatives, their production and use |
RU2127274C1 (ru) * | 1992-09-25 | 1999-03-10 | Эли Лилли Энд Компани | СПОСОБ ПОЛУЧЕНИЯ 5-ЗАМЕЩЕННЫХ ПИРРОЛО (2,3-α)ПИРИМИДИНОВ |
US5416211A (en) * | 1992-09-25 | 1995-05-16 | Eli Lilly And Company | Process for preparing 5-substituted pyrrolo-[2,3-d]pyrimidines |
CZ283345B6 (cs) * | 1993-05-24 | 1998-03-18 | Eli Lilly And Company | Způsob přípravy v poloze 5 substituovaného derivátu pyrrolo [2,3-d]pyrimidinu |
-
1998
- 1998-09-18 CA CA002304656A patent/CA2304656A1/en not_active Abandoned
- 1998-09-18 HU HU0003954A patent/HUP0003954A3/hu unknown
- 1998-09-18 CN CNB98809553XA patent/CN1213998C/zh not_active Expired - Fee Related
- 1998-09-18 ID IDW20000531A patent/ID24165A/id unknown
- 1998-09-18 EA EA200000359A patent/EA002452B3/ru not_active IP Right Cessation
- 1998-09-18 CZ CZ20050764A patent/CZ301563B6/cs not_active IP Right Cessation
- 1998-09-18 IL IL13519098A patent/IL135190A/xx active IP Right Grant
- 1998-09-18 AU AU94937/98A patent/AU740087B2/en not_active Ceased
- 1998-09-18 JP JP2000513828A patent/JP2001518459A/ja active Pending
- 1998-09-18 BR BR9812524-9A patent/BR9812524A/pt not_active Application Discontinuation
- 1998-09-18 WO PCT/US1998/019560 patent/WO1999016742A1/en not_active Application Discontinuation
- 1998-09-18 CN CNB031490409A patent/CN1246295C/zh not_active Expired - Fee Related
- 1998-09-18 KR KR1020007003219A patent/KR20010030712A/ko not_active Application Discontinuation
- 1998-09-18 PL PL339452A patent/PL196216B1/pl unknown
- 1998-09-18 TR TR2000/01220T patent/TR200001220T2/xx unknown
- 1998-09-18 NZ NZ503600A patent/NZ503600A/en unknown
- 1998-09-18 UA UA2000031700A patent/UA53742C2/uk unknown
- 1998-09-24 US US09/160,129 patent/US6013828A/en not_active Expired - Fee Related
-
2000
- 2000-03-24 NO NO20001554A patent/NO314456B1/no not_active Application Discontinuation
-
2005
- 2005-03-17 NO NO2005007C patent/NO2005007I2/no unknown
Also Published As
Publication number | Publication date |
---|---|
TR200001220T2 (tr) | 2001-05-21 |
JP2001518459A (ja) | 2001-10-16 |
IL135190A0 (en) | 2001-05-20 |
EA002452B3 (ru) | 2018-02-28 |
AU740087B2 (en) | 2001-11-01 |
US6013828A (en) | 2000-01-11 |
NZ503600A (en) | 2001-08-31 |
UA53742C2 (uk) | 2003-02-17 |
EA002452B1 (ru) | 2002-04-25 |
NO2005007I2 (no) | 2008-02-11 |
NO314456B1 (no) | 2003-03-24 |
HUP0003954A3 (en) | 2002-12-28 |
CZ301563B6 (cs) | 2010-04-14 |
NO2005007I1 (no) | 2005-04-04 |
CN1475477A (zh) | 2004-02-18 |
KR20010030712A (ko) | 2001-04-16 |
CA2304656A1 (en) | 1999-04-08 |
CN1213998C (zh) | 2005-08-10 |
AU9493798A (en) | 1999-04-23 |
IL135190A (en) | 2005-03-20 |
WO1999016742A1 (en) | 1999-04-08 |
ID24165A (id) | 2000-07-13 |
BR9812524A (pt) | 2000-07-25 |
NO20001554D0 (no) | 2000-03-24 |
CN1271338A (zh) | 2000-10-25 |
NO20001554L (no) | 2000-05-24 |
PL196216B1 (pl) | 2007-12-31 |
PL339452A1 (en) | 2000-12-18 |
CN1246295C (zh) | 2006-03-22 |
EA200000359A1 (ru) | 2000-10-30 |
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