Dw. Gordon et J. Steele, REDUCTIVE ALKYLATION ON A SOLID-PHASE - SYNTHESIS OF A PIPERAZINEDIONE COMBINATORIAL LIBRARY, Bioorganic & medicinal chemistry letters, 5(1), 1995, pp. 47-50
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.