CN109219611A - 达格列净中间体的晶型及其制备方法 - Google Patents

达格列净中间体的晶型及其制备方法 Download PDF

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CN109219611A
CN109219611A CN201780033823.6A CN201780033823A CN109219611A CN 109219611 A CN109219611 A CN 109219611A CN 201780033823 A CN201780033823 A CN 201780033823A CN 109219611 A CN109219611 A CN 109219611A
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crystal form
preparation
compound
formula
dapagliflozin
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CN109219611B (zh
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李响
余俊
于海洲
王进家
何雷
杜祖银
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04—Carbocyclic radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

公开了一种达格列净中间体的晶型及其制备方法，具体公开了达格列净中间体(2S,3R,4S,5S,6R)‑2‑(4‑氯‑3‑(4‑乙氧基苄基)苯基)‑2‑乙氧基‑6‑(甲基羟基)四氢‑2H‑吡喃‑3,4,5‑三醇的晶型及其制备方法。其优点在于，能够将中间体高度提纯，得到纯度达99.3％以上的样品，对于提高达格列净的质量有重要的意义，并且制备工艺简单，适宜工业化的生产。

Description

PCT国内申请，说明书已公开。

Claims (13)

  1. PCT国内申请，权利要求书已公开。
CN201780033823.6A 2016-07-22 2017-07-21 达格列净中间体的晶型及其制备方法 Active CN109219611B (zh)

Applications Claiming Priority (3)

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CN201610587582.7A CN107641139A (zh) 2016-07-22 2016-07-22 达格列净中间体的晶型及其制备方法
CN2016105875827 2016-07-22
PCT/CN2017/093833 WO2018014866A1 (zh) 2016-07-22 2017-07-21 达格列净中间体的晶型及其制备方法

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CN109219611A true CN109219611A (zh) 2019-01-15
CN109219611B CN109219611B (zh) 2022-03-29

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US (1) US10836786B2 (zh)
EP (1) EP3489250A4 (zh)
JP (1) JP2019521151A (zh)
KR (1) KR20190031485A (zh)
CN (2) CN107641139A (zh)
BR (1) BR112019000521A2 (zh)
MX (1) MX2019000582A (zh)
WO (1) WO2018014866A1 (zh)

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Publication number Priority date Publication date Assignee Title
WO2020151672A1 (zh) * 2019-01-23 2020-07-30 苏州科睿思制药有限公司 一种达格列净晶型及其制备方法和用途
EP4114365A1 (en) 2020-03-05 2023-01-11 KRKA, d.d., Novo mesto Pharmaceutical composition comprising sglt2 inhibitor
CN111748004A (zh) * 2020-06-30 2020-10-09 药璞(上海)医药科技有限公司 一种高纯度达格列净中间体的晶型及其制备方法
CN114539334A (zh) * 2021-03-31 2022-05-27 浙江美诺华药物化学有限公司 一种达格列净中间体化合物晶型及其制备方法
CN116813675B (zh) * 2023-08-23 2023-11-24 北京远大九和药业有限公司 一种化合物晶型及其制备、组合物和用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013152654A1 (en) * 2012-04-10 2013-10-17 Theracos, Inc. Process for preparation of benzylbenzene sodium-dependent glucose cotransporter 2 (sglt2) inhibitors
CN104109179A (zh) * 2013-04-16 2014-10-22 杭州华东医药集团生物工程研究所有限公司 一类c-芳基葡萄糖苷衍生物、制备方法及其用途
WO2015132803A2 (en) * 2014-03-06 2015-09-11 Msn Laboratories Private Limited Process for the preparation of (1s)-1,5-anhydro-1-c-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-d-glucitol and its solvate thereof
CN105481915A (zh) * 2014-09-19 2016-04-13 北京万生药业有限责任公司 一种sglt-2抑制剂化合物的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2295422A3 (de) * 2004-03-16 2012-01-04 Boehringer Ingelheim International GmbH Glucopyranosylsubstituierte Benzolderivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
US9193751B2 (en) * 2012-04-10 2015-11-24 Theracos, Inc. Process for the preparation of benzylbenzene SGLT2 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013152654A1 (en) * 2012-04-10 2013-10-17 Theracos, Inc. Process for preparation of benzylbenzene sodium-dependent glucose cotransporter 2 (sglt2) inhibitors
CN104109179A (zh) * 2013-04-16 2014-10-22 杭州华东医药集团生物工程研究所有限公司 一类c-芳基葡萄糖苷衍生物、制备方法及其用途
WO2015132803A2 (en) * 2014-03-06 2015-09-11 Msn Laboratories Private Limited Process for the preparation of (1s)-1,5-anhydro-1-c-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-d-glucitol and its solvate thereof
CN105481915A (zh) * 2014-09-19 2016-04-13 北京万生药业有限责任公司 一种sglt-2抑制剂化合物的制备方法

Also Published As

Publication number Publication date
CN107641139A (zh) 2018-01-30
WO2018014866A1 (zh) 2018-01-25
US10836786B2 (en) 2020-11-17
BR112019000521A2 (pt) 2019-04-24
KR20190031485A (ko) 2019-03-26
EP3489250A4 (en) 2020-02-26
CN109219611B (zh) 2022-03-29
MX2019000582A (es) 2019-04-01
JP2019521151A (ja) 2019-07-25
US20190284220A1 (en) 2019-09-19
EP3489250A1 (en) 2019-05-29

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