Journal
ACS COMBINATORIAL SCIENCE
Volume 21, Issue 10, Pages 705-715Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.9b00144
Keywords
combinatorial chemistry; multicomponent reactions; domino process; carbodiimide; dihydroorotic acid
Funding
- Politecnico di Milano
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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 N-u-substituted-N-4-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.
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