Nhwa Pharma. Corporation

Shanhai Institute of Pharmaceutical Industry

Shanghai Institute of Pharmaceutical Industry

Yanqin Ma

Guisen Zhang

Jianqi Li

Guan Zhong Wang

Xiangping Yang

Shixia Zhou

Lin Guo

Yuan Yuan Zhang

Xiangqing Xu

Shicheng Liu

Daopeng Chen

Liang Chen

Wenhua Ji

Shuming Hu

Guan Wang

A process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy- 1-naphthy)ethyl]phthalimide is provided and inclues reacting 7-methoxy-1-naphthyl ethanol (III) with benzenesulfonyl chloride to obtain 7-methoxy-1 -naphthylethyl benzene sulfonate (IV), which is reacted with potassium phthalimide to produce N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II); and subjecting N-[2-(7-methoxy-1-naphthy)ethyl]phthalimide (II) to alkaline hydrolysis and acetylation, to obtain agomelatine.

Process for the manufacture of agomelatine and its intermediate

The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects. 

Aralkyl piperidine derivatives and their uses as antalgic or ataractic agent

The use of aryl piperazines of formula (I) in manufacturing a medicament for treating acute pain, neuropathic pain or receptive nociceptive pain in mammals including human beings is disclosed. 

Use of aryl piperazine derivatives in manufacturing medicants for treating pain

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Xuzhou, China

Yanqin Ma