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A process featuring a sequential multicomponent reaction followed by regioselective post-cyclization strategy was implemented for the facile synthesis of N,N'-disubstituted dihydroorotic acid amides in very mild condition. We obtained, for… Click to show full abstract
A process featuring a sequential multicomponent reaction followed by regioselective post-cyclization strategy was implemented for the facile synthesis of N,N'-disubstituted dihydroorotic acid amides in very mild condition. 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.
Journal Title: ACS combinatorial science
Year Published: 2019
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