JP7098651B2 - エリグルスタット及びその中間化合物の合成方法 - Google Patents

エリグルスタット及びその中間化合物の合成方法 Download PDF

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JP7098651B2
JP7098651B2 JP2019552046A JP2019552046A JP7098651B2 JP 7098651 B2 JP7098651 B2 JP 7098651B2 JP 2019552046 A JP2019552046 A JP 2019552046A JP 2019552046 A JP2019552046 A JP 2019552046A JP 7098651 B2 JP7098651 B2 JP 7098651B2
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compound
protecting group
hydrogen
hydroxy protecting
reaction
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JP2020511508A5 (https=
JP2020511508A (ja
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リウ，ユ
ユ，グアンネン
ツェン，チーグオ
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チョーチアン オウスン ファーマシューティカル カンパニー リミテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/24—Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds
    • C07C209/26—Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with hydrogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • 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)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
JP2019552046A 2017-03-21 2017-10-16 エリグルスタット及びその中間化合物の合成方法 Active JP7098651B2 (ja)

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CN201710169305.9A CN106967042B (zh) 2017-03-21 2017-03-21 依利格鲁司他的合成方法及其中间体化合物
CN201710169305.9 2017-03-21
PCT/CN2017/106348 WO2018171173A1 (zh) 2017-03-21 2017-10-16 依利格鲁司他的合成方法及其中间体化合物

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US (2) US9988364B1 (https=)
EP (2) EP4417605A3 (https=)
JP (2) JP7098651B2 (https=)
KR (1) KR102547559B1 (https=)
CN (2) CN106967042B (https=)
ES (1) ES2986115T3 (https=)
HR (1) HRP20241128T1 (https=)
HU (1) HUE068098T2 (https=)
PT (1) PT3611171T (https=)
WO (1) WO2018171173A1 (https=)

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Publication number Priority date Publication date Assignee Title
CN106967042B (zh) 2017-03-21 2020-08-14 浙江奥翔药业股份有限公司 依利格鲁司他的合成方法及其中间体化合物
US20200306225A1 (en) * 2017-10-27 2020-10-01 Msn Laboratories Private Limited, R&D Center Stable n-((1r,2r)-1-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl) octanamide (2r,3r)-2,3-dihydroxysuccinate premix and process for preparation thereof
WO2020020365A1 (zh) * 2018-07-27 2020-01-30 中国医学科学院药物研究所 制备光活依格鲁特的方法
CN110759885B (zh) * 2018-07-27 2021-10-22 中国医学科学院药物研究所 制备光活依格鲁特的方法
CN110878079A (zh) * 2018-12-31 2020-03-13 北京启慧生物医药有限公司 一种高纯度依利格鲁司他的制备方法
CN110256321B (zh) * 2019-06-12 2021-05-28 山东省医学科学院药物研究所（山东省抗衰老研究中心、山东省新技术制药研究所） (2r,3s,4s)-4-氨基-2-十四烷基吡咯烷-3-醇的制备方法及其应用
CN113893346B (zh) * 2020-06-22 2022-11-18 四川大学华西医院 Gcs抑制剂在制备治疗可卡因成瘾的药物中的用途
CN112125805B (zh) * 2020-09-11 2022-10-18 北京红惠新医药科技有限公司 水溶性厚朴酚衍生物及和厚朴酚衍生物和其中间体的制备方法、和相关的单羟基保护中间体
CN113880819B (zh) * 2021-09-18 2024-09-20 浙江大学医学院附属第一医院 立他司特的制备方法及其中间体化合物
CN114456089B (zh) * 2022-03-29 2023-05-23 南昌航空大学 一种路易斯酸促进的烯烃和肟酯与胺的三组分反应方法

Citations (4)

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JP2005255686A (ja) 2001-07-16 2005-09-22 Genzyme Corp Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成
CN104557851A (zh) 2015-02-10 2015-04-29 苏州明锐医药科技有限公司 依鲁司他的制备方法
CN105646442A (zh) 2015-10-27 2016-06-08 北京凯莱天成医药科技有限公司 一种依利格鲁司他的制备方法
CN106349210A (zh) 2016-08-24 2017-01-25 北京阳光诺和药物研究有限公司 一种制备酒石酸艾力骨司坦的方法

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WO2017068496A1 (en) 2015-10-20 2017-04-27 Dr. Reddy' S Laboratories Limited Improved process for the preparation of eliglustat and its salts
CN106349310B (zh) 2016-08-26 2019-06-11 内蒙古嘉宝仕生物科技股份有限公司 甲氨基阿维菌素苯甲酸盐的制备方法
CN106967042B (zh) * 2017-03-21 2020-08-14 浙江奥翔药业股份有限公司 依利格鲁司他的合成方法及其中间体化合物

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JP2005255686A (ja) 2001-07-16 2005-09-22 Genzyme Corp Ｕｄｐ−グルコース：ｎ−アシルスフィンゴシングルコシルトランスフェラーゼインヒビターの合成
CN104557851A (zh) 2015-02-10 2015-04-29 苏州明锐医药科技有限公司 依鲁司他的制备方法
CN105646442A (zh) 2015-10-27 2016-06-08 北京凯莱天成医药科技有限公司 一种依利格鲁司他的制备方法
CN106349210A (zh) 2016-08-24 2017-01-25 北京阳光诺和药物研究有限公司 一种制备酒石酸艾力骨司坦的方法

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ES2986115T3 (es) 2024-11-08
JP2022058564A (ja) 2022-04-12
CN106967042A (zh) 2017-07-21
EP3611171A1 (en) 2020-02-19
US11697644B2 (en) 2023-07-11
KR102547559B1 (ko) 2023-06-26
JP7307823B2 (ja) 2023-07-12
EP4417605A3 (en) 2025-03-12
CN106967042B (zh) 2020-08-14
HRP20241128T1 (hr) 2024-11-22
WO2018171173A1 (zh) 2018-09-27
US20200031808A1 (en) 2020-01-30
CN110461826A (zh) 2019-11-15
PT3611171T (pt) 2024-09-04
EP3611171B1 (en) 2024-06-12
KR20190140927A (ko) 2019-12-20
US9988364B1 (en) 2018-06-05
HUE068098T2 (hu) 2024-12-28
CN110461826B (zh) 2023-08-25
JP2020511508A (ja) 2020-04-16
EP4417605A2 (en) 2024-08-21
EP3611171A4 (en) 2021-03-03

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