361458-05-1Relevant articles and documents
Solid-phase synthesis of piperazinones via disrupted ugi condensation
Treder, Adam P.,Tremblay, Marie-Claude,Yudin, Andrei K.,Marsault, Eric
, p. 4674 - 4677 (2014)
The first application of aziridine aldehyde dimers in solid-phase synthesis is reported. The solid-supported disrupted Ugi condensation between an aziridine aldehyde dimer, isonitrile, and backbone-anchored amino acids delivered N-acyl aziridine intermediates, which were reacted with nucleophiles to yield the corresponding piperazinones. Subsequent cleavage from the resin provided a diverse set of 2,3,6-trisubstituted piperazinones starting from various amino acids, aziridine aldehydes, and nucleophiles.
