Department of Food, Environmental and Nutritional Sciences , Università degli Studi di Milano , via Celoria 2 , 20133 Milano , Italy.
Department of Chemistry, Material and Chemical Engineer "Giulio Natta" , Politecnico di Milano , via Mancinelli 7 , 20131 Milano , Italy.
ACS Comb Sci. 2019 Oct 14;21(10):705-715. doi: 10.1021/acscombsci.9b00144. Epub 2019 Sep 5.
A process featuring a sequential multicomponent reaction followed by a regioselective postcyclization strategy was implemented for the facile synthesis of ,'-disubstituted dihydroorotic acid amides under mild conditions. We obtained, for the first time, a library of 29 derivatives, encompassing 19 -substituted--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.
我们实施了一个具有顺序多组分反应随后进行区域选择性后环化策略的过程，以在温和条件下轻松合成 -'二取代的二氢乳清酸酰胺。我们首次获得了 29 种衍生物的文库，其中包括 19 种 -取代的 -二氢乳清酰基-4-氨基苯丙氨酸衍生物，这是促性腺激素释放激素拮抗剂 Degarelix 的关键残基。相应的产物是由易于获得的起始原料制备的，具有良好至优异的产率和广泛的底物范围。
