JP7748948B2 - メルファランの合成方法 - Google Patents

メルファランの合成方法

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Publication number
JP7748948B2
JP7748948B2 JP2022538939A JP2022538939A JP7748948B2 JP 7748948 B2 JP7748948 B2 JP 7748948B2 JP 2022538939 A JP2022538939 A JP 2022538939A JP 2022538939 A JP2022538939 A JP 2022538939A JP 7748948 B2 JP7748948 B2 JP 7748948B2
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JP
Japan
Prior art keywords
formula
amino
group
phenylalanine
melphalan
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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.)
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JP2022538939A
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English (en)
Japanese (ja)
Other versions
JP2023508071A5 (enExample
JP2023508071A (ja
Inventor
ピエトロ アレグリーニ、
アンドレア ボネッティ、
マルコ モリナリ、
アンドレア ジャンビーニ、
Original Assignee
インデナ エッセ ピ ア
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Publication of JP2023508071A publication Critical patent/JP2023508071A/ja
Publication of JP2023508071A5 publication Critical patent/JP2023508071A5/ja
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Classifications

    • 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
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2022538939A 2019-12-23 2020-12-21 メルファランの合成方法 Active JP7748948B2 (ja)

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 (3)

Publication Number Publication Date
JP2023508071A JP2023508071A (ja) 2023-02-28
JP2023508071A5 JP2023508071A5 (enExample) 2023-12-18
JP7748948B2 true JP7748948B2 (ja) 2025-10-03

Family

ID=70009318

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2022538939A Active JP7748948B2 (ja) 2019-12-23 2020-12-21 メルファランの合成方法

Country Status (8)

Country Link
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB750155A (en) 1953-03-17 1956-06-13 Nat Res Dev Substituted alanines
US3032585A (en) 1954-12-03 1962-05-01 Nat Res Dev Process for the production of p-bis-(2-chloroethyl)-aminophenylalanine
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
DE4026115A1 (de) * 1990-08-17 1992-02-20 Consortium Elektrochem Ind Verfahren zur herstellung von 1-alkylisochinolinderivaten
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
Donald A. TOMALIA et al.，"The synthesis andreactions of β‐substituted ethyl sulfates"，Journal of Heterocyclic Chemistry，1972年08月，Vol. 9, No. 4，p.891-894，DOI: 10.1002/jhet.5570090424

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
CN114845991B (zh) 2024-05-07
US20230286901A1 (en) 2023-09-14
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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