Synthesis of 3H??and 14C??labelled CP??88,059: A potent atypical antipsychotic agent

HR Howard, KD Shenk, TA Smolarek…

Index: Howard; Shenk; Smolarek; Marx; Windels; Roth Journal of Labelled Compounds and Radiopharmaceuticals, 1994 , vol. 34, # 2 p. 117 - 125

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Citation Number: 11

Abstract

Abstract The syntheses of 3 H-and 14 C-labelled CP-88,059 [ie, 5-(2-(4-(1, 2-benzisothiazol- 3-yl) piperazinyl) ethyl)-6-chloro-1, 3-dihydro-2H-indol-2-one] are described. CP-88,059 (5b) is a combined D 2/5-HT 2 antagonist currently undergoing clinical evaluation as an antipsychotic agent with reduced potential for induction of EPS in schizophrenic patients. Displacement of bromine from the 7-position of the benzisothiazole moiety, by reductive ...