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Allenylidene Induced 1,2‐Metalate Rearrangement of Indole‐Boronates: Diastereoselective Access to Highly Substituted Indolines

Amit Kumar Simlandy, M. Kevin Brown

2021Angewandte Chemie International Edition20 citationsDOIOpen Access PDF

Abstract

A process to achieve 1,2-metalate rearrangements of indole boronate as a way to access substituted indolines in high diastereoselectivities is presented. The reaction involves the generation of a Cu-allenylidene, which is sufficiently electrophilic to induce the 1,2-metalate rearrangement. The scope of the reaction is evaluated as well as further transformations of the product.

Topics & Concepts

Indole testScope (computer science)ChemistryElectrophileCatalysisMedicinal chemistryStereochemistryOrganic chemistryComputer scienceProgramming languageCatalytic C–H Functionalization MethodsOrganoboron and organosilicon chemistryAsymmetric Synthesis and Catalysis