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-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.
Solanki, Pavankumar V.,Uppelli, Sekhar Babu,Pandit, Bhushan S.,Mathad, Vijayavitthal T.
A PROCESS FOR THE PREPARATION OF ILOPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
The present invention relates to a new process for the preparation of 1- [4-[3-[4-(6-fluoro- 1,2-benzisoxazol-3-yl)- l-piperidinyl]propoxy]-3- methoxyphenyl]- ethanone (Iloperidone) and salts thereof. The synthetic process comprises the reaction between i
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(2012/12/13)
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