Abstract
AbstractActinomycin 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‐aziridine‐carbonyl‐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 with respect to physical properties and biological activity.
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