化学
对映体药物
区域选择性
戒指(化学)
组合化学
立体化学
全合成
炔烃
有机化学
对映选择合成
催化作用
作者
Yi Lin,F. R. N. Schneider,Kelly J. Eberle,Debora Chiodi,Hakobu Nakamura,Solomon H. Reisberg,Jason Chen,Masato Saito,Phil S. Baran
摘要
A concise, modular synthesis of the novel antibiotic darobactin A is disclosed. The synthesis successfully forges the hallmark strained macrocyclic ring systems in a sequential fashion. Key transformations include two atroposelective Larock-based macrocyclizations, one of which proceeds with exquisite regioselectivity despite bearing an unprotected alkyne. The synthesis is designed with medicinal chemistry considerations in mind, appending key portions of the molecule at a late stage. Requisite unnatural amino acid building blocks are easily prepared in an enantiopure form using C-H activation and decarboxylative cross-coupling tactics.
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