CN111511722A - 一种制备噁拉戈利中间体的方法及其组合物 - Google Patents

一种制备噁拉戈利中间体的方法及其组合物 Download PDF

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Publication number
CN111511722A
CN111511722A CN201880081586.5A CN201880081586A CN111511722A CN 111511722 A CN111511722 A CN 111511722A CN 201880081586 A CN201880081586 A CN 201880081586A CN 111511722 A CN111511722 A CN 111511722A
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formula
compound
organic layer
group
stirring
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CN111511722B (zh
Inventor
苏虎
郭效文
梁玉坤
石凯强
杨锦涛
何康
陶安平
黄鲁宁
安建国
陈茜
顾虹
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Shanghai Kesheng Pharmaceutical Research And Development Co ltd
Zhejiang Huahai Pharmaceutical Co Ltd
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Shanghai Kesheng Pharmaceutical Research And Development Co ltd
Zhejiang Huahai Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

本发明涉及一种噁拉戈利钠中间体(式IV)的制备方法,所述方法通过下面的路线制备,该方法操作简捷安全,收率良好,同时环境污染小,有很好的经济效应,适宜工业生产,

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。
CN201880081586.5A 2017-12-27 2018-12-25 一种制备噁拉戈利中间体的方法及其组合物 Active CN111511722B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017114452525 2017-12-27
CN201711445252.5A CN109970663B (zh) 2017-12-27 2017-12-27 一种制备噁拉戈利中间体的方法
PCT/CN2018/123468 WO2019128983A1 (zh) 2017-12-27 2018-12-25 一种制备噁拉戈利中间体的方法及其组合物

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CN111511722A true CN111511722A (zh) 2020-08-07
CN111511722B CN111511722B (zh) 2022-01-18

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US (1) US11365178B2 (zh)
EP (1) EP3733650A4 (zh)
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WO (1) WO2019128983A1 (zh)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109970663B (zh) * 2017-12-27 2023-04-11 上海科胜药物研发有限公司 一种制备噁拉戈利中间体的方法
CN110501446B (zh) * 2019-08-28 2021-12-17 江苏海岸药业有限公司 一种噁拉戈利钠原料及其合成中间体的分析方法
CN110938038A (zh) * 2019-11-14 2020-03-31 上海星酶生物科技有限公司 一种c13h10f4n2o2的制备工艺
CN111333586A (zh) * 2020-02-19 2020-06-26 诚达药业股份有限公司 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN111333548B (zh) * 2020-04-10 2022-04-26 江苏海悦康医药科技有限公司 1-(2-氟-6-(三氟甲基)苄基)脲的制备方法
CN111995584B (zh) * 2020-09-01 2022-03-29 常州工学院 恶拉格利中间体的制备方法
CN112159358B (zh) * 2020-10-26 2023-08-18 上海朴颐化学科技有限公司 一种噁拉戈利中间体的制备方法
CN115677598A (zh) * 2022-11-11 2023-02-03 南通常佑药业科技有限公司 一种合成嘧啶二酮类化合物的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1819829A (zh) * 2003-07-07 2006-08-16 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
WO2009062087A1 (en) * 2007-11-07 2009-05-14 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
CN109970663A (zh) * 2017-12-27 2019-07-05 上海科胜药物研发有限公司 一种制备噁拉戈利中间体的方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1819829A (zh) * 2003-07-07 2006-08-16 纽罗克里生物科学有限公司 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物
WO2009062087A1 (en) * 2007-11-07 2009-05-14 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
CN109970663A (zh) * 2017-12-27 2019-07-05 上海科胜药物研发有限公司 一种制备噁拉戈利中间体的方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
LIREN ZHAO等: "5-Aryluracils as potent GnRH antagonists—Characterization of atropisomers", 《BIOORG. MED. CHEM. LETT》 *

Also Published As

Publication number Publication date
CN109970663A (zh) 2019-07-05
CN111511722B (zh) 2022-01-18
WO2019128983A1 (zh) 2019-07-04
CN109970663B (zh) 2023-04-11
EP3733650A4 (en) 2021-09-29
EP3733650A1 (en) 2020-11-04
US20200369625A1 (en) 2020-11-26
US11365178B2 (en) 2022-06-21

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