Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

Autor: Gail L. Wrigley, Shaun M. Fillery, Barry M. Hayter, Paula Perkins, Jason Grant Kettle, Emma J. Williams, Peter Mark Smith, Mandy L. Crowther, Rebecca J. Burton, Peter Robins, Neal J. Fazakerley, Caroline Anne McMillan
Rok vydání: 2013
Předmět:
Zdroj: Tetrahedron Letters. 54:6900-6904
ISSN: 0040-4039
Popis: The highly regioselective Buchwald–Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodology is robust and provides a facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald–Hartwig amination at higher temperature to enable rapid exploration of the chemical space at C-4 and to provide a library of 2,4-bisaminopyridines.
Databáze: OpenAIRE