Data di Pubblicazione:
2019
Citazione:
Multicomponent Approach to Libraries of Substituted Dihydroorotic Acid Amides / M.C. Bellucci, A. Sacchetti, A. Volonterio. - In: ACS COMBINATORIAL SCIENCE. - ISSN 2156-8952. - 21:10(2019 Oct), pp. 705-715. [10.1021/acscombsci.9b00144]
Abstract:
A process featuring a sequential multicomponent reaction followed by a regioselective postcyclization strategy was implemented for the facile synthesis of N,N′-disubstituted dihydroorotic acid amides under mild conditions. We obtained, for the first time, a library of 29 derivatives, encompassing 19 Nα-substituted-N4-dihydroorotyl-4-aminophenylalanine derivatives, a key residue of gonadotropin-releasing hormone antagonist Degarelix. The corresponding products were prepared from easily accessible starting materials in good to excellent yields with broad substrate scope.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
carbodiimide; combinatorial chemistry; dihydroorotic acid; domino process; multicomponent reactions
Elenco autori:
M.C. Bellucci, A. Sacchetti, A. Volonterio
Link alla scheda completa: