Guangdong Key Laboratory of Chiral Molecule and Drug Discovery, School of Pharmaceutical Sciences , Sun Yat-sen University , Guangzhou 510006 , China.
J Org Chem. 2019 Dec 6;84(23):15331-15342. doi: 10.1021/acs.joc.9b02350. Epub 2019 Nov 20.
A zinc-catalyzed intermolecular alkyne-carbonyl metathesis reaction of ynamides with isatins followed by an amide to ester conversion has been developed, which produces the indolone derivatives with a fully substituted alkene species in good to high yields. The salient features of this reaction include the following: mild reaction conditions, an inexpensive zinc catalyst, a broad substrate scope, the excellent regiocontrol and stereoselectivity, and amenable to the gram scale.
发展了一种锌催化的炔酰胺与靛红的分子间炔羰基复分解反应，接着进行酰胺到酯的转化，以良好至高的收率得到了具有完全取代烯烃的吲哚啉衍生物。该反应的显著特点包括：温和的反应条件、廉价的锌催化剂、广泛的底物范围、优异的区域选择性和立体选择性，以及适合克级规模。
