W. Yi, Z. Heng, Yang Yi-hong
2010
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Journal
Fine Chemical Intermediates
Abstract
1,2-Benzoisothiazole-3-piperazine(2) was synthesized from 3-chloro-1,2-benzoisothiazole and piperazine.5-(2-Chloroacetyl)-6-chloro-indole ketone(3) was synthesized from 6-chloro-indole ketone and chloroacetyl chloride by Friedel-crafts acylation.Reduction of 3 by sodium borohydride gave 5-(2-chloroethyl)-6-chloro-indole ketone(4).Combination of 2 and 4 in aqueous solution of NaI / NaCO3 produced ziprasidone(1) in overall yield of 50.5%.The structures were confirmed by IR and 1H NMR.