CN114845991B - 合成美法仑的方法 - Google Patents

合成美法仑的方法 Download PDF

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Publication number
CN114845991B
CN114845991B CN202080089455.9A CN202080089455A CN114845991B CN 114845991 B CN114845991 B CN 114845991B CN 202080089455 A CN202080089455 A CN 202080089455A CN 114845991 B CN114845991 B CN 114845991B
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China
Prior art keywords
formula
group
amino
phenylalanine
melphalan
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Chinese (zh)
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CN114845991A (zh
Inventor
P·阿莱格里尼
A·博内蒂
M·莫利纳里
A·甘比尼
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Yidina Co ltd
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Yidina Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
    • C07C227/20—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters by hydrolysis of N-acylated amino-acids or derivatives thereof, e.g. hydrolysis of carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202080089455.9A 2019-12-23 2020-12-21 合成美法仑的方法 Active CN114845991B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT102019000025348A IT201900025348A1 (it) 2019-12-23 2019-12-23 Procedimento per la sintesi di melfalan
IT102019000025348 2019-12-23
PCT/EP2020/087443 WO2021130163A1 (en) 2019-12-23 2020-12-21 A process for the synthesis of melphalan

Publications (2)

Publication Number Publication Date
CN114845991A CN114845991A (zh) 2022-08-02
CN114845991B true CN114845991B (zh) 2024-05-07

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CN202080089455.9A Active CN114845991B (zh) 2019-12-23 2020-12-21 合成美法仑的方法

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US (2) US11787761B2 (enExample)
EP (1) EP4081503B1 (enExample)
JP (1) JP7748948B2 (enExample)
CN (1) CN114845991B (enExample)
ES (1) ES3040894T3 (enExample)
HU (1) HUE073252T2 (enExample)
IT (1) IT201900025348A1 (enExample)
WO (1) WO2021130163A1 (enExample)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114315618A (zh) * 2021-12-04 2022-04-12 浙江恒腾福生物科技集团有限公司 一种合成美法仑的制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3032584A (en) * 1953-03-17 1962-05-01 Nat Res Dev p-bis-(2-chloroethyl) aminophenylalanine and the process for the production thereof
US4255326A (en) * 1979-03-30 1981-03-10 Eastman Kodak Company Nitrogen and/or sulfur containing heterocyclic azo dyes with aniline, tetrahydroquinoline and benzomorpholine couplers having sulfate group
US4267104A (en) * 1979-06-14 1981-05-12 Eastman Kodak Company Dyes from selected substituted aniline diazo components and aniline couplers containing sulfate ester groups
US5272270A (en) * 1990-08-17 1993-12-21 Consortium Fur Elektrochemische Industrie Gmbh Process for the preparation of 1-alkylisoquinoline derivatives
WO2014191426A1 (en) * 2013-05-31 2014-12-04 Farmabios S.P.A. Process for the purification of melphalan
CN107935875A (zh) * 2017-12-27 2018-04-20 兆科药业（广州）有限公司 一种美法仑的合成方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3032585A (en) 1954-12-03 1962-05-01 Nat Res Dev Process for the production of p-bis-(2-chloroethyl)-aminophenylalanine
CN100491339C (zh) 2007-04-20 2009-05-27 苏州市立德化学有限公司 一种抗肿瘤药物美法仑的合成工艺
US8575385B2 (en) 2008-03-20 2013-11-05 Navinta Llc Process of making optically pure melphalan

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3032584A (en) * 1953-03-17 1962-05-01 Nat Res Dev p-bis-(2-chloroethyl) aminophenylalanine and the process for the production thereof
US4255326A (en) * 1979-03-30 1981-03-10 Eastman Kodak Company Nitrogen and/or sulfur containing heterocyclic azo dyes with aniline, tetrahydroquinoline and benzomorpholine couplers having sulfate group
US4267104A (en) * 1979-06-14 1981-05-12 Eastman Kodak Company Dyes from selected substituted aniline diazo components and aniline couplers containing sulfate ester groups
US5272270A (en) * 1990-08-17 1993-12-21 Consortium Fur Elektrochemische Industrie Gmbh Process for the preparation of 1-alkylisoquinoline derivatives
WO2014191426A1 (en) * 2013-05-31 2014-12-04 Farmabios S.P.A. Process for the purification of melphalan
CN107935875A (zh) * 2017-12-27 2018-04-20 兆科药业（广州）有限公司 一种美法仑的合成方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
"The Synthesis and Reactions of P-Substituted Ethyl Sulfates";Donald A. To mlia等;《journal of heterocyclic chemistry》;第9卷(第4期);第891-894页 *

Also Published As

Publication number Publication date
US12077484B2 (en) 2024-09-03
US20230094970A1 (en) 2023-03-30
EP4081503C0 (en) 2025-07-30
ES3040894T3 (en) 2025-11-05
IT201900025348A1 (it) 2021-06-23
WO2021130163A1 (en) 2021-07-01
US20230286901A1 (en) 2023-09-14
JP7748948B2 (ja) 2025-10-03
HUE073252T2 (hu) 2026-01-28
EP4081503B1 (en) 2025-07-30
JP2023508071A (ja) 2023-02-28
US11787761B2 (en) 2023-10-17
CN114845991A (zh) 2022-08-02
EP4081503A1 (en) 2022-11-02

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