Ra. Smith et al., SOLID-PHASE SYNTHESIS OF A LIBRARY OF PIPERAZINEDIONES AND DIAZEPINEDIONES VIA KAISER OXIME RESIN, Bioorganic & medicinal chemistry letters, 8(17), 1998, pp. 2369-2374
A combinatorial library of piperazinediones has been prepared by autom
ated parallel solid-phase synthesis. The five-step reaction protocol m
akes use of Kaiser oxime resin, to enable cleavage from the polymeric
support concomitant with an intramolecular displacement reaction, unde
r very mild conditions. The methodology was also successfully extended
to the preparation of the seven-membered ring homologs, diazepinedion
es. (C) 1998 Elsevier Science Ltd. All rights reserved.