REDUCTIVE ALKYLATION ON A SOLID-PHASE - SYNTHESIS OF A PIPERAZINEDIONE COMBINATORIAL LIBRARY

The synthesis of a prototype trisubstituted piperazinedione combinator ial library of 1,000 compounds has been achieved from three precursor sets - two sets of ten a-amino acids and one set of ten aldehydes. A s odium triacetoxyborohydride-mediated reductive alkylation was crucial to the success of the multi-step synthesis on resin. This protocol rep resents a new method to augment compound files rapidly with novel hete rocyclic entities for high-speed screening.