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1. WO2022088573 - METHOD FOR PREPARING PYROTINIB

Publication Number WO/2022/088573
Publication Date 05.05.2022
International Application No. PCT/CN2021/079228
International Filing Date 05.03.2021
IPC
C07D 401/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
CPC
C07B 2200/07
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
07Optical isomers
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
Applicants
  • 苏州富士莱医药股份有限公司 SUZHOU FUSHILAI PHARMACEUTICAL CO., LTD [CN]/[CN]
Inventors
  • 张晓红 ZHANG, Xiaohong
  • 王永兴 WANG, Yongxing
  • 孙晓彤 SUN, Xiaotong
  • 韩秋月 HAN, Qiuyue
Agents
  • 北京德崇智捷知识产权代理有限公司 JW IP LAW FIRM
Priority Data
202011176723.929.10.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) METHOD FOR PREPARING PYROTINIB
(FR) PROCÉDÉ DE PRÉPARATION DE PYROTINIB
(ZH) 一种吡咯替尼的制备方法
Abstract
(EN) A method for preparing pyrotinib, which belongs to the technical field of chemical synthesis of medicines. The method comprises the following steps: 1. preparing R,E-N-(-2-hydroxy-4-nitrophenyl)-3-(-1-methylpyrrolidin-2-yl)acrylamide; 2. preparing (R,E)-N-(2-ethoxy-4-nitrophenyl)-3-(1-methylpyrrolidin-2-yl)acrylamide; 3. preparing (R,E)-N-(4-amino-2-ethoxyphenyl)-3-(1-methylpyrrolidin-2-yl)acrylamide; 4. preparing (2E)-N-(4-amino-3-cyano-7-ethoxyquinolin-6-yl)-3-[(2R)-1-methylpyrrolidin-2-yl]acrylamide; and 5. preparing pyrotinib. The method has the advantages of the raw materials being readily available and the process being simple, economical and environmentally friendly. The method is beneficial for improving and controlling the quality of a final product bulk drug.
(FR) L'invention concerne un procédé de préparation de pyrotinib, se rapportant au domaine technique de la synthèse chimique de médicaments. Le procédé comprend les étapes suivantes consistant à : 1. La préparation de R,E-N-(-2-hydroxy-4-nitrophényl)-3-(-1-méthylpyrrolidin-2-yl)acrylamide ; 2. la préparation de (R,E)-N-(2-éthoxy-4-nitrophényl)-3-(1-méthylpyrrolidin-2-yl)acrylamide ; 3. la préparation de (R,E)-N-(4-amino-2-éthoxyphényl)-3-(1-méthylpyrrolidin-2-yl)acrylamide ; 4. la préparation de (2E)-N-(4-amino-3-cyano-7-éthoxyquinolin-6-yl)-3-[(2R)-1-méthylpyrrolidin-2-yl]acrylamide ; et 5. la préparation de pyrotinib. Le procédé présente les avantages de matières premières facilement disponibles et le procédé est simple, économique et respectueux de l'environnement. Le procédé est avantageux dans l'amélioration et la régulation de la qualité d'un médicament en vrac produit final.
(ZH) 一种吡咯替尼的制备方法,属于药物化学合成技术领域。步骤:1、制备R,E-N-(2-羟基-4-硝基苯基)-3-(1-甲基吡咯烷-2-基)丙烯酰胺;2、制备(R,E)-N-(2-乙氧基-4-硝基苯基)-3-(1-甲基吡咯烷-2-基)丙烯酰胺;3、制备(R,E)-N-(4-氨基-2-乙氧基苯基)-3-(1-甲基吡咯烷-2-基)丙烯酰胺;4、制备(2E)-N-(4-氨基-3-氰基-7-乙氧基喹啉-6-基)-3-[(2R)-1-甲基吡咯烷-2-基]丙烯酰胺;5、制备吡咯替尼。优点:原料易得、工艺简洁和经济环保,有利于提高并控制终产品原料药的质量。
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