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US 2010/0076196 A1Published application
Process for the preparation of iloperidone
OwnerMiklós Vértessyinventor
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Abstract
A process for the preparation of crystalline 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]-ethanone (Iloperidone), which comprises the reaction between 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole and 3-methoxy-4-hydroxy-acetophenone.
Claims14
A procedure to prepare Iloperidone and salts thereof comprising the following steps:
- a. reacting 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole with 3-methoxy-4-hydroxy-acetophenone in the presence of a base, using an organic solvent;
- b. pouring the reaction medium into water;
- c. extracting the aqueous phase with ethyl acetate and separating the layers;
- d. washing the organic phase with aqueous sodium hydroxide solution, with acidified sodium chloride saturated solution and with water;
- e. distilling off the solvent under reduced pressure;
- f. crystallizing the product from an appropriate solvent;
- g. recrystallizing the product from an appropriate solvent;
- and
- h. preparing a solution of the free base into a solvent and adding the desired acid in the same solvent in order to obtain the corresponding salt.
6 more elements
A crystalline form of 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]ethanone (Iloperidone).
A procedure to prepare Iloperidone and salts thereof comprising the following steps:
- a. reacting 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole with 3-methoxy-4-hydroxy-acetophenone in the presence of a base, using an organic solvent, and
- b. extracting the reaction product.
Dependencies are inferred from the claim text.