State Key Laboratory of High-efficiency Utilization of Coal and Green Chemical Engineering, National Demonstration Center for Experimental Chemistry Education, School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021, China.
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xue Yuan Rd. 38, Beijing 100191, China.
J Org Chem. 2022 Mar 4;87(5):3691-3700. doi: 10.1021/acs.joc.1c02622. Epub 2022 Feb 9.
An efficient Cp*Rh(III)-catalyzed regioselective C(sp)-H mono- and dialkynylation of thioamides was described. This reaction was performed under mild conditions in high yields (up to 98%) with a broad substrate scope. Significantly, the versatility of this method was further demonstrated by controlled mono- and dialkynylation. Application of this protocol in the late stage functionalization of two drug molecules (Adapalene and Amoxapine) was also demonstrated.
一种高效的 Cp*Rh(III)-催化的硫酰胺 C(sp)-H 单和二炔基化反应被描述。该反应在温和条件下进行，以高产率（高达 98%）和广泛的底物范围进行。值得注意的是，该方法的多功能性通过控制的单和二炔基化进一步得到了证明。该方案在两种药物分子（阿达帕林和阿莫沙平）的后期功能化中的应用也得到了证明。
