Improved and Efficient Process for the Production of Highly Pure Iloperidone: A Psychotropic Agent

The present work describes an improved and highly efficient process for the synthesis of iloperidone (1), an antipsychotic agent, which is free from potential impurities. The synthesis comprises N-alkylation of 1-(4-(3-chloropropoxy)-3-methoxyphenyl)ethanone (4) with 6-fluoro-3-piperidin-4-yl-1,2-be...

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Bibliographic Details
Published in:Organic process research & development 2014-02, Vol.18 (2), p.342-348
Main Authors: Solanki, Pavankumar V, Uppelli, Sekhar Babu, Pandit, Bhushan S, Mathad, Vijayavitthal T
Format: Article
Language:English
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Summary:The present work describes an improved and highly efficient process for the synthesis of iloperidone (1), an antipsychotic agent, which is free from potential impurities. The synthesis comprises N-alkylation of 1-(4-(3-chloropropoxy)-3-methoxyphenyl)ethanone (4) with 6-fluoro-3-piperidin-4-yl-1,2-benzisoxazole hydrochloride (5) in a mixture of water and heptane as solvent and sodium hydroxide as a base in the presence of tetrabutylammonium bromide as a phase transfer catalyst to yield iloperidone (1) with a yield of around 95% and a purity of 99.80% by HPLC. The present work also describes the optimization details performed to achieve the process attributes responsible for high yield and purity.
ISSN:1083-6160
1520-586X
DOI:10.1021/op400335p