Department of Chemistry, University of Pittsburg, Pittsburg, PA 15260 U.S.A.
Abstract:
The synthesis of N4-peptidyl- derivatives of ara-C (1) is described. In these derivatives, the active drug is released by an intramolecular cyclization process with formation of a six-membered heterocycle. No enzymatic or solvolytic conversion is necessary. NMR studies of the rates of cyclization is basic and acidic environment are discussed.