CN104736540B - 培美曲塞及其赖氨酸盐的制备方法 - Google Patents

培美曲塞及其赖氨酸盐的制备方法 Download PDF

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Publication number
CN104736540B
CN104736540B CN201380041935.8A CN201380041935A CN104736540B CN 104736540 B CN104736540 B CN 104736540B CN 201380041935 A CN201380041935 A CN 201380041935A CN 104736540 B CN104736540 B CN 104736540B
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pemetrexed
salt
water
lysine
acid
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Chinese (zh)
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CN104736540A (zh
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F·博纳科尔西
F·卡尔瓦尼
F·帕斯奎
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Berlin Chemie AG
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Berlin Chemie AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380041935.8A 2012-08-08 2013-08-08 培美曲塞及其赖氨酸盐的制备方法 Active CN104736540B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITRM2012A000398 2012-08-08
IT000398A ITRM20120398A1 (it) 2012-08-08 2012-08-08 Procedimento di sintesi pemetrexed e suo sale di lisina.
PCT/IB2013/056497 WO2014024164A1 (en) 2012-08-08 2013-08-08 Process for the preparation of pemetrexed and lysin salt thereof

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CN104736540A CN104736540A (zh) 2015-06-24
CN104736540B true CN104736540B (zh) 2017-08-25

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Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107641124A (zh) * 2016-07-22 2018-01-30 上海创诺制药有限公司 一种培美曲塞二酸新晶型及其制备方法
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
JP7490239B2 (ja) 2018-02-07 2024-05-27 エル.イー.エー.エフ. ホールディングス グループ エルエルシー ガンマポリグルタミン酸化ペメトレキセドおよびその使用
JP7491572B2 (ja) 2018-02-07 2024-05-28 エル.イー.エー.エフ. ホールディングス グループ エルエルシー アルファポリグルタミン酸化ペメトレキセドおよびその使用
CN110128428A (zh) * 2018-02-09 2019-08-16 鲁南制药集团股份有限公司 培美曲塞丙氨酸盐
CN110128426B (zh) * 2018-02-09 2021-12-14 鲁南制药集团股份有限公司 培美曲塞谷氨酸盐
CN110128427A (zh) * 2018-02-09 2019-08-16 鲁南制药集团股份有限公司 培美曲塞缬氨酸盐
CN111333658A (zh) * 2020-05-06 2020-06-26 贵州联科中贝制药科技有限公司 一种培美曲塞二钠水合物的制备方法

Citations (4)

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CN1087910A (zh) * 1992-09-25 1994-06-15 伊莱利利公司 5-取代的吡咯并[2,3-d]嘧啶的制备方法
EP2301909A1 (en) * 2008-05-30 2011-03-30 Shanghai Cdymax Pharmaceuticals Co., Ltd Processes for preparing pemetrexed disodium and its intermediate,4-(4-carbomethoxyphenyl)butanal
CN102344452A (zh) * 2010-07-22 2012-02-08 凯米股份公司 合成培美曲塞二钠盐的新方法
WO2012056285A1 (en) * 2010-10-25 2012-05-03 Fresenius Kabi Oncology Ltd. An improved process for the preparation of pemetrexed

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US5112991A (en) 1988-10-31 1992-05-12 Mitsui Toatsu Chemicals Incorporated Process for the preparation of an organo-substituted sodium aluminum hydride
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
IL96531A (en) 1989-12-11 1995-08-31 Univ Princeton History of Acid N- (Diomeric-H1-Pyrolo] D-2,3 [Pyrimidine-3-Ilacyl (-glutamic, preparation and pharmaceutical preparations containing them)
US5416211A (en) 1992-09-25 1995-05-16 Eli Lilly And Company Process for preparing 5-substituted pyrrolo-[2,3-d]pyrimidines
DE19725647A1 (de) 1997-06-18 1998-12-24 Basf Ag Cyclopenta[I]phenanthren-Metallkomplex-Katalysatorsysteme
ZA987550B (en) 1997-09-26 2000-02-21 Lilly Co Eli Processes and intermediates useful to make antifolates.
HU229704B1 (en) 2000-02-25 2014-05-28 Lilly Co Eli A novel crystalline form of n-[4-[2-(2-amino-4,7-dihydro-4-oxo-3h-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and process for its preparation
KR101101443B1 (ko) * 2006-08-14 2012-01-03 시코르, 인크. 페메트렉세드의 중간체의 제조 방법
EP1934226A2 (en) * 2006-08-14 2008-06-25 Sicor, Inc. Highly pure pemetrexed diacid and processes for the preparation thereof
EP2598148A4 (en) 2010-07-28 2014-05-28 Eagle Pharmaceuticals Inc PHARMACEUTICAL COMPOSITIONS WITH PEMETREXED WITH EXTENDED STORAGE STABILITY

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CN1087910A (zh) * 1992-09-25 1994-06-15 伊莱利利公司 5-取代的吡咯并[2,3-d]嘧啶的制备方法
EP2301909A1 (en) * 2008-05-30 2011-03-30 Shanghai Cdymax Pharmaceuticals Co., Ltd Processes for preparing pemetrexed disodium and its intermediate,4-(4-carbomethoxyphenyl)butanal
CN102344452A (zh) * 2010-07-22 2012-02-08 凯米股份公司 合成培美曲塞二钠盐的新方法
WO2012056285A1 (en) * 2010-10-25 2012-05-03 Fresenius Kabi Oncology Ltd. An improved process for the preparation of pemetrexed

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A New and Efficient Synthesis of Pyrrolo[2,3-d]pyrimidine Anticancer Agents: Alimta (LY231514, MTA), Homo-Alimta,TNP-351, and Some Aryl 5-Substituted Pyrrolo[2,3-d]pyrimidines;Edward C. Taylor,等;《J. Org. Chem.》;20031122;第68卷(第26期);第9938-9947页 *
A Novel Synthetic Approach to Pyrrolo[2,3-d]pyrimidine Antifolates;Tetauo Miwa,等;《Journal of Organic Chemistry》;19931231;第58卷(第7期);第1696-1701页 *
A Practical Synthesis of Multitargeted Antifolate LY231514;Charles J. Barnett,等;《Organic Process Research & Development》;19990430;第3卷(第3期);第184-188页 *

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Publication number Publication date
LT2882753T (lt) 2016-12-12
RU2609006C2 (ru) 2017-01-30
TW201412741A (zh) 2014-04-01
MX362858B (es) 2019-02-20
IN2015DN00833A (cg-RX-API-DMAC10.html) 2015-06-12
KR20150045458A (ko) 2015-04-28
DK2882753T3 (en) 2017-01-16
RS55515B1 (sr) 2017-05-31
SMT201600474B (it) 2017-03-08
EP2882753A1 (en) 2015-06-17
EP2882753B1 (en) 2016-10-05
WO2014024164A1 (en) 2014-02-13
KR102288417B1 (ko) 2021-08-11
SMT201600474T1 (it) 2017-03-08
BR112015002429A2 (pt) 2017-07-04
AU2013301156A1 (en) 2015-02-05
ZA201501549B (en) 2016-01-27
MX2015001712A (es) 2015-08-14
CN104736540A (zh) 2015-06-24
HRP20170011T1 (hr) 2017-03-10
CY1118514T1 (el) 2017-07-12
ES2607890T3 (es) 2017-04-04
TWI609017B (zh) 2017-12-21
AU2013301156B2 (en) 2017-08-31
PL2882753T3 (pl) 2017-04-28
RU2015108042A (ru) 2016-09-27
HUE032304T2 (en) 2017-09-28
PT2882753T (pt) 2016-12-27
SI2882753T1 (sl) 2017-02-28
HK1209426A1 (en) 2016-04-01
BR112015002429A8 (pt) 2019-07-30
ITRM20120398A1 (it) 2014-02-09

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