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AGOMELATINE INTERMEDIATES AND PREPARATION METHOD THEREOF
专利权人:
르 라보레또레 쎄르비에르;LES LABORATOIRES SERVIER
发明人:
ZHANG PENG,장, 펭,HUANG YU,후앙, 유,YUAN ZHEDONG,유안, 체동,SHAN HANBIN,샨, 한빈,YU XIONG,유, 슝
申请号:
KR1020137000375
公开号:
KR1020130028134A
申请日:
2011.06.08
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine. Said reaction processes are greatly simplified, with the reaction yield being improved and the difficulty in purification of previous method being overcome, as compare with the previous technique for preparation of agomelatine. Typically, the yield of the present invention is over 70%.본원에는 아고멜라틴의 제조를 위한 중간체 화합물 및 이의 제조 방법이 제공된다. 또한, 두 개의 신규한 중간체 화합물이 제공된다. 이러한 방법은 조작이 간단하고, 잘 조절되고, 산업적 생산에 적합하며, 복잡한 작업, 예컨대, 정류 및 컬럼 크로마토그래피 분리 없이 순도가 높다. 또한, 본 발명의 두 개의 신규한 중간체 자체를 제조하는 방법은 간단하고, 수율이 높다.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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