Hydrogen Peroxide → 3-{4-[2-(6-Chloro-2-oxo-2,3-dihydro-1H-indol-5-yl)ethyl]piperazin-1-yl}-1H-1lambda~4~,2-benzothiazol-1-one

Participants

Reaction Steps

To a solution of ziprasidone made as described in Example 1 (0.70 g, 1.7 mmol) in acetonitrile is added 30% H2O2 (1.7 mmol). After stirring for 24 hours at room temperature, the reaction mixture is cooled, filtered, and evaporated. The residue is chromatographed on silica gel, eluting the by-products with ethyl acetate (1 L) and the product with 4% methanol in ethyl acetate (1.5 L). The product fractions are evaporated, taken up in methylene chloride, and precipitated by addition of ether saturated with HCl; the solid is filtered and washed with ether, dried, and washed with acetone.

Provenance & Evidence