Henan Engineering Research Center of Functional Materials and Catalytic Reaction, College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004, China.
J Org Chem. 2022 Nov 4;87(21):14005-14015. doi: 10.1021/acs.joc.2c01637. Epub 2022 Oct 9.
A facile and effective tandem reaction of ynones and methyl salicylates was developed to obtain a broad range of 3-acyl chromones in moderate-to-excellent yields. This protocol underwent a Michael addition and cyclization process, which exhibited easily accessible substrates, broad substrate scope, and high regioselectivity under mild and transition-metal-free conditions. Moreover, gram-scale reaction and further chemical transformation of the products were also further studied.
我们开发了一种简便有效的 ynones 和甲基水杨酸盐串联反应,以中等至优异的收率获得了广泛的 3-酰基色酮。该方案经历了迈克尔加成和环化过程,在温和条件和无过渡金属条件下具有易于获得的底物、广泛的底物范围和高区域选择性。此外,还进一步研究了克级反应和产物的进一步化学转化。