The solid phase synthesis of 1,3,4,7-tetrasubstituted perhydro-1,4-dia
zepine-2,5-diones is described. Starting from the resin-bound tBu este
r of aspartic acid and employing reductive alkylation and amide format
ion, 40 diazepines have been synthesized in good yield and high purity
. The general nature of this approach permits not only large numbers o
f individual diazepines to be prepared, but also combinatorial librari
es. (C) 1997 Elsevier Science Ltd.