Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, KU Leuven, Celestijnenlaan 200F, Leuven 3001, Belgium.
College of Chemistry and Chemical Engineering & Shanghai Engineering Research Center of Textile Chemistry and Cleaner Production, Shanghai University of Engineering Science, Shanghai 201620, China.
J Org Chem. 2021 Oct 15;86(20):14036-14043. doi: 10.1021/acs.joc.1c00537. Epub 2021 Apr 23.
1,4-Diamino-2-butynes display both chemical and physiological properties. Here a highly efficient synthesis avenue to generate unsymmetric 1,4-diamino-2-butynes has been developed by microwave-assisted Cu(I)-catalyzed cross-A-coupling/decarboxylative coupling of two different amines, formaldehyde, and propiolic acid through a domino process. This multicomponent reaction provides a series of target products in moderate to good yields with high chemoselectivity.
1,4-二氨基-2-丁炔具有化学和生理双重性质。在此，我们开发了一条高效的合成途径，通过微波辅助的铜（I）催化的两种不同胺、甲醛和丙炔酸的交叉 A-偶联/脱羧偶联的级联反应，来生成不对称的 1,4-二氨基-2-丁炔。该多组分反应以中等到良好的收率和高化学选择性提供了一系列目标产物。
