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1. The Synthesis of 3,3-Dimethyl Aza- and Diazaindolines Using a Palladium-Catalysed Intramolecular Reductive Cyclisation

Author

Colin Hogg, Julian Northern, Michael Reader, Christopher N. Johnson, Alistair Meek, Martyn Frederickson, Gary Patrick Reid, and James Edward Harvey Day

Subjects
Chemistry, Intramolecular force, Organic Chemistry, chemistry.chemical_element, Halogenation, Alkylation, Medicinal chemistry, Catalysis, Palladium
Abstract

A range of azaindolines was prepared in three steps from heterocyclic amines using halogenation, alkylation with 3-bromo-2-methylpropene, and a palladium-catalysed reductive cyclisation. The chemistry proved applicable to a multigram-scale operation.

Published
2015
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