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1. WO2022000868 - INTERMEDIATE FOR SYNTHESIZING CAMPTOTHECIN DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF

Publication Number WO/2022/000868
Publication Date 06.01.2022
International Application No. PCT/CN2020/122298
International Filing Date 21.10.2020
IPC
C07C 233/25 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
16having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
24with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
25having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 233/33 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
01having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
30having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
33with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
C07C 231/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07D 491/16 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
12in which the condensed system contains three hetero rings
16Peri-condensed systems
C07D 491/22 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
22in which the condensed system contains four or more hetero rings
Applicants
  • 上海皓元生物医药科技有限公司 SHANGHAI HAOYUAN MEDCHEMEXPRESS CO., LTD. [CN]/[CN]
Inventors
  • 张宏伟 ZHANG, Hongwei
  • 张大明 ZHANG, Daming
  • 马涛 MA, Tao
  • 朱琦伟 ZHU, Qiwei
  • 周治国 ZHOU, Zhiguo
  • 梅魁 MEI, Kui
  • 郑保富 ZHENG, Baofu
  • 高强 GAO, Qiang
  • 袁海玲 YUAN, Hailing
Agents
  • 北京尚诚知识产权代理有限公司 SHANGCHENG & PARTNERS
Priority Data
202010593916.828.06.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) INTERMEDIATE FOR SYNTHESIZING CAMPTOTHECIN DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
(FR) INTERMÉDIAIRE DE SYNTHÈSE D'UN DÉRIVÉ DE CAMPTOTHÉCINE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 用于合成喜树碱衍生物的中间体及其制备方法和用途
Abstract
(EN) Provided are an intermediate for synthesizing a camptothecin derivative, a preparation method therefor, and the use thereof. An intermediate A can be obtained from 3-fluoro-4-methylaniline by means of acylation, bromination, and cross-coupling reactions. The intermediate A can be used for preparing an intermediate B to further prepare exatecan mesylate. The intermediate compound B can be obtained from the intermediate A by means of a rearrangement reaction, and exatecan mesylate can be obtained from the intermediate compound B by means of deprotection for acetamido and amino at the ɑ site, a condensation reaction, and a hydrolysis reaction. The reaction starting materials have a low price, the reaction conditions of each step are moderate, the operation is simple, and the yield is high, such that the intermediate is suitable for industrial production.
(FR) L'invention concerne un intermédiaire de synthèse d'un dérivé de camptothécine, son procédé de préparation et son utilisation. Un intermédiaire A peut être obtenu à partir de 3-fluoro-4-méthylaniline par des réactions d'acylation, de bromation et de couplage croisé. L'intermédiaire A peut être utilisé pour préparer un intermédiaire B afin de préparer par la suite du mésylate d'exatécan. Le composé intermédiaire B peut être obtenu à partir de l'intermédiaire A au moyen d'une réaction de réarrangement, et le mésylate d'exatécan peut être obtenu à partir du composé intermédiaire B au moyen d'une déprotection pour un acétamido et un amino au niveau du site ɑ, d'une réaction de condensation et d'une réaction d'hydrolyse. Les matières premières de réaction ont un faible prix, les conditions de réaction de chaque étape sont modérées, le mode opératoire est simple, et le rendement est élevé, de telle sorte que l'intermédiaire est approprié pour une production industrielle.
(ZH) 提供了一种用于合成喜树碱衍生物的中间体及其制备方法和用途。中间体A可由3-氟-4-甲基苯胺经过酰化、溴代、交叉偶联反应得到。该中间体A可以用于制备中间体B进而制备伊喜替康甲磺酸盐。中间体化合物B可由中间体A经过重排反应得到;伊喜替康甲磺酸盐可由化合物B经过ɑ位上乙酰氨基、氨基脱保护、缩合反应、水解反应得到。所述反应起始物价格低廉,各步反应条件温和,操作简便,收率高,适合工业化生产。
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