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1. CN111470998 - Intermediate for synthesizing camptothecin derivative as well as preparation method and application thereof

Office
China
Application Number 202010593916.8
Application Date 28.06.2020
Publication Number 111470998
Publication Date 31.07.2020
Grant Number 111470998
Grant Date 25.09.2020
Publication Kind B
IPC
C07C 233/25
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
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
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
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
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
CPC
C07C 233/25
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 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07C 231/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
02from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07D 491/16
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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
12in which the condensed system contains three hetero rings
16Peri-condensed systems
C07D 491/22
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 C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
22in which the condensed system contains four or more hetero rings
C07C 2601/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
04with a four-membered ring
Applicants MEDCHEMEXPRESS CHINA CO., LTD.
上海皓元生物医药科技有限公司
Inventors ZHANG HONGWEI
张宏伟
ZHANG DAMING
张大明
MA TAO
马涛
ZHU QIWEI
朱琦伟
ZHOU ZHIGUO
周治国
MEI KUI
梅魁
ZHENG BAOFU
郑保富
GAO QIANG
高强
YUAN HAILING
袁海玲
Title
(EN) Intermediate for synthesizing camptothecin derivative as well as preparation method and application thereof
(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) The invention relates to the technical field of organic compound synthesis, in particular to an intermediate for synthesizing a camptothecin derivative as well as a preparation method and applicationof the intermediate. An intermediate A can be obtained by acylation, bromination and cross coupling reaction of 3-fluoro-4-methylaniline. The intermediate A can be used for preparing an intermediate Bso as to further prepare Exatecan mesylate. The intermediate compound B can be obtained by rearrangement reaction of the intermediate A; Exatecan mesylate can be obtained by subjecting the intermediate compound B to alpha-site acetamido and amino deprotection, condensation reaction and hydrolysis reaction. The method has the advantages of low price of reaction initiators, mild reaction conditionsof each step, simplicity and convenience in operation, high yield and suitability for industrial production.
(ZH) 本发明涉及有机化合物合成技术领域,尤其是涉及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。本发明的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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