State Key Laboratory of Applied Organic Chemistry, Lanzhou University , Lanzhou 730000, P.R. China.
Org Lett. 2016 Aug 19;18(16):4016-9. doi: 10.1021/acs.orglett.6b01711. Epub 2016 Aug 10.
A highly diastereoselective dearomatization of indoles via palladium-catalyzed decarboxylative alkynyl termination was developed. This protocol provides dissimilar tetracyclic and tetrasubstituted indoline scaffolds bearing congested stereocenters, which led to operationally simple conditions, short time, and broad substrate scope. Additionally, this reaction system could be scaled to gram quantities in a satisfactory yield and diastereoselectivity.
发展了一种钯催化脱羧炔基终止的吲哚高非对映选择性去芳构化反应。该方法提供了具有拥挤立体中心的不同四环和四取代吲哚啉骨架,反应条件操作简单、反应时间短、底物适用范围广。此外,该反应体系可以在满意的收率和非对映选择性下放大到克级规模。