The Improved Process for the Preparation of Iloperidone

Zhen Hua Shang, Qian Qian Chu,Jing Ha, Chen Hong An, Pan Wang

Advanced Materials Research(2015)

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摘要
The main object of the present invention is to provide an improved process for the preparation of Iloperidone, which would be more simple, economical and easy to implement on large scale preparation. In this paper, 1,3-difluorobenzene and 1-(4-hydroxy-3-methoxyphenyl) ethanone are starting materials. And then tartaric acid is added. The key intermediate (Z)-4-(2,4-difluorobenzoyl) piperidine oxime is obtained through stereoselectivity. With the key intermediate and 1-(4-(3-chloropropoxy)-3-methoxyphenyl) ethanone, the target product is obtained directly under the condition of catalyst.
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