Abstract

The Mizoroki–Heck reaction is one of the key C–C bond-forming processes in organic synthesis. A prominent variant, which has found broadest application in targeted complex molecule synthesis, is the asymmetric intramolecular Mizoroki–Heck reaction. This methodology has outshone another powerful facet of Mizoroki–Heck chemistry, which has been prospering in recent years, namely directed Mizoroki–Heck reactions. Initially designed to achieve high regiocontrol in intermolecular reactions, this technique has recently been extended to highly diastereoselective and even enantioselective substrate-directed inter- as well as intramolecular Mizoroki–Heck reactions. This summary delineates the evolution of this chemistry from regio- to diastereo- and finally, enantioselective transformations.

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