Solid phase synthesis of 1-aminohydantoin libraries

Article abstract of DOI:10.1016/S0040-4039(98)01009-0

The solid support synthesis of a series of I-aminohydantoins based on a diverse set of hydrazino amino acid, aldehydes, and amines is described. The method involves the construction of resin attached hydrazino acid precursors, followed by subsequent derivatization, and then cyclizative cleavage off the resin. Overall yields vary per example between 15 and 60%, and the samples are suitable for biological evaluations without further purification.