Synthesis of iloperidone
10.7644/j.issn.1674-9960.2015.04.009
- VernacularTitle:伊潘立酮的合成研究
- Author:
Bei WANG
;
Heng ZHANG
;
Yihong YANG
;
Hong CHEN
;
Shuang CAO
- Publication Type:Journal Article
- Keywords:
iloperidone;
antipsychotic agents;
synthesis
- From:
Military Medical Sciences
2015;(4):271-275
- CountryChina
- Language:Chinese
-
Abstract:
Objective To optimize the synthesis process of iloperidone 1 for industrial production.Methods Piperi-dine-4-carboxylic acid, acetic acid and acetic anhydride were used as starting materials to generate 2 via amidation, Friedel-Crafts acylation, hydration, oximation, intramolecular cyclization and salification.Compound 2 was treated with 4-(3-chloropropoxy)-3-methoxyphenylethanone through condensation to afford iloperidone.The target compound 1 was prepared with an overall yield of 34.9%.Results and Conclusion Such factors as the ratio of the raw materials, the catalyst, reactive time were investigated and optimized to make the reaction conditions mild and easy to control with less side effects.The structure has been confirmed by IR, 1 H-NMR and MS.
