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Total Synthesis of (−)-Gardmultimine A

Peiqi Chen, Hesi Yang, Hao Zhang, Wei Chen, Zheng Zhang, Jing Zhang, Huilin Li, Xiaolei Wang, Xingang Xie, Xuegong She

2020Organic Letters32 citationsDOI

Abstract

The first total synthesis of Gardneria oxindole alkaloid (−)-gardmultimine A has been achieved in 19 steps from d-tryptophan in a fully stereocontrolled manner. This synthesis features (1) an Ir-catalyzed regioselective C–H borylation/oxidation sequence to introduce the C12 methoxyl group, (2) a stereocontrolled oxidative rearrangement of indole to construct the spirooxindole motif, and (3) an Au(I)-catalyzed transannular Conia-ene-type 6-exo-dig cyclization to establish the azabicyclo[2.2.2]octane skeleton and the exocyclic E-alkene with exclusive stereoselectivity.

Topics & Concepts

ChemistryOxindoleRegioselectivityStereoselectivityBorylationStereochemistryTotal synthesisIndole testAlkeneIndole alkaloidOctaneEne reactionCatalysisOrganic chemistryAlkylArylCatalytic C–H Functionalization MethodsAlkaloids: synthesis and pharmacologyMarine Sponges and Natural Products