EA202091962A1 - Способ производства 4-боронфенилаланина - Google Patents

Способ производства 4-боронфенилаланина

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Publication number
EA202091962A1
EA202091962A1 EA202091962A EA202091962A EA202091962A1 EA 202091962 A1 EA202091962 A1 EA 202091962A1 EA 202091962 A EA202091962 A EA 202091962A EA 202091962 A EA202091962 A EA 202091962A EA 202091962 A1 EA202091962 A1 EA 202091962A1
Authority
EA
Eurasian Patent Office
Prior art keywords
boronphenylalanine
amino acid
production method
groups
hydrogenolysis
Prior art date
Application number
EA202091962A
Other languages
English (en)
Inventor
Петр Царадник
Иржи Малинак
Ян Кочи
Original Assignee
Оцука Фармасьютикал Ко., Лтд.
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
Application filed by Оцука Фармасьютикал Ко., Лтд. filed Critical Оцука Фармасьютикал Ко., Лтд.
Publication of EA202091962A1 publication Critical patent/EA202091962A1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/027Organoboranes and organoborohydrides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B47/00Formation or introduction of functional groups not provided for in groups C07B39/00 - C07B45/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B49/00Grignard reactions
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B51/00Introduction of protecting groups or activating groups, not provided for in the preceding groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00Purification; Separation; Stabilisation; Use of additives
    • C07B63/02Purification; Separation; Stabilisation; Use of additives by treatment giving rise to a chemical modification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/02Magnesium compounds
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Данное изобретение относится к способу производства 4-боронфенилаланина (БФА) из 4-йодфенилаланина, в котором все функциональные группы аминокислоты защищены бензиловым способом защиты и в котором применяют галогенид изопропилмагния, стабилизированный связывающим основанием, и затем конденсируют полученный реагент Гриньяра со сложным эфиром борной кислоты. Конечная стадия реакции, каталитический гидрогенолиз или трансферный гидрогенолиз защитных групп аминокислоты, проходит после гидролиза боронатных эфирных групп.
EA202091962A 2018-02-20 2019-02-19 Способ производства 4-боронфенилаланина EA202091962A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862632862P 2018-02-20 2018-02-20
PCT/JP2019/005984 WO2019163738A1 (en) 2018-02-20 2019-02-19 Method of 4-boronophenylalanine production

Publications (1)

Publication Number Publication Date
EA202091962A1 true EA202091962A1 (ru) 2020-11-06

Family

ID=65812368

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202091962A EA202091962A1 (ru) 2018-02-20 2019-02-19 Способ производства 4-боронфенилаланина

Country Status (9)

Country Link
US (1) US11098067B2 (ru)
EP (1) EP3755681B1 (ru)
JP (1) JP7273854B2 (ru)
KR (1) KR102635698B1 (ru)
CN (1) CN111741939A (ru)
EA (1) EA202091962A1 (ru)
ES (1) ES2929196T3 (ru)
PL (1) PL3755681T3 (ru)
WO (1) WO2019163738A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20230416280A1 (en) * 2020-11-13 2023-12-28 Stella Pharma Corporation Method for producing 4-borono-l-phenylalanine and intermediate thereof
FR3120630B1 (fr) * 2021-03-09 2023-02-10 Orano Chimie Enrichissement Composé boré utile pour la séparation isotopique du bore, son procédé de synthèse et ses utilisations
CN116925119A (zh) * 2022-03-30 2023-10-24 海南普利制药股份有限公司 一种4-10硼酸-l-苯丙氨酸中间体的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000212185A (ja) * 1999-01-14 2000-08-02 Ajinomoto Co Inc パラボロノフェニルアラニン誘導体の製造方法
EP2865682B1 (en) 2013-10-28 2016-10-26 Taiwan Biotech Co., Ltd. Process for preparing 4-Borono-L-Phenylalanine
CN104961756A (zh) * 2015-06-16 2015-10-07 上海应用技术学院 一种(S)-Boc-4-二羟基硼酰苯丙氨酸的制备方法
WO2017028751A1 (zh) 2015-08-14 2017-02-23 南京中硼联康医疗科技有限公司 L-bpa的制备方法

Also Published As

Publication number Publication date
US20200392163A1 (en) 2020-12-17
KR20200123441A (ko) 2020-10-29
KR102635698B1 (ko) 2024-02-14
JP2021514008A (ja) 2021-06-03
PL3755681T3 (pl) 2022-11-28
US11098067B2 (en) 2021-08-24
ES2929196T3 (es) 2022-11-25
EP3755681B1 (en) 2022-09-07
EP3755681A1 (en) 2020-12-30
WO2019163738A1 (en) 2019-08-29
CN111741939A (zh) 2020-10-02
JP7273854B2 (ja) 2023-05-15

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