Abstract

Abstract Actinomycin D (C1) has been synthesized by a route involving the ester formation between two peptide fragments, (2S,3S)-1-(2-nitro-3-benzyloxy-4-methylbenzoyl)-3-methyl-2-aziridinecarbonyl-d-valylproline t-butyl ester and N-benzyloxycarbonylsarcosyl-N-methylvaline, via a ring-opening reaction of aziridine. Cyclization, followed by reduction and oxidation, gave actinomycin D (C1). The synthetic actinomycin D (C1) was indistinguishable from natural substance as regards physical properties and biological activity.

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