Synthesis of Metabolites of the Cerebroprotecting Agent 7-Hydroxy-1-[[[4-(3-methoxyphenyl)-1-piperazinyl]acetyl]amino]-2, 2, 4, 6-tetramethylindan (OPC-14117)

Abstract

A hydroxylated metabolite (5a) of 7-hydroxy-1-[[[4-(3-methoxyphenyl)-1-piperazinyl]acetyl]amino]-2, 2, 4, 6-tetramethylindan (OPC-14117), which is a novel cerebroprotective agent with central nervous system-stimulating activity, was synthesized by use of a model cytochrome P-450 system. In order to confirm the structure of this compound it was prepared by another route. The structures of several metabolites (5a, 7 and 8) were identified by means of comparisons with the synthetic compounds.