Synthesis of N-(1-Keto-) and N-(1-Hydroxy-5-Indansulfonyl)-N′-(4-Chlorophenyl)Urea, Two Major Metabolites of the Antitumor Agent Sulofenur (LY186641)

Abstract

A brief (3–4 step), large-scale synthesis of two major metabolites of the antitumor agent sulofenur was developed. The required intermediate, 1-keto-5-indansulfonamide, was prepared in only two steps, utilizing a novel method for converting an aromatic chloride to a sulfonamide.