Method for preparation of iloperidone and crystallization method thereof
AssigneeZhejiang Huahai Pharmaceutical Co., Ltd.
InventorsShiwei Zhou, Feng Jian
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Abstract
A method for preparation of iloperidone is provided which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride with 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone in an inorganic alkaline aqueous solution. A crystallization method of iloperidone is also provided which comprises adding seed crystal to the iloperidone solution in ethyl acetate, and then iloperidone crystal is obtained with high purity by controlling the temperature and the stirring speed.
Claims12
A method for preparing iloperidone represented by formula (I) which chemical name is 1-(4-(3-(4-(6-fluoro-1,2-benzoisoxazole-3-yl)piperidinyl)propoxyl)-3-methoxyphenyl)ethyl ketone:
- characterized in that it comprises reacting raw material 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride represented by formula (V)
- with raw material 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone represented by formula (IV)
- in an inorganic alkaline aqueous solution to prepare iloperidone represented by formula (I).
Dependencies are inferred from the claim text.