Title of article :
Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries
Author/Authors :
Burton، نويسنده , , Rebecca J. and Crowther، نويسنده , , Mandy L. and Fazakerley، نويسنده , , Neal J. and Fillery، نويسنده , , Shaun M. and Hayter، نويسنده , , Barry M. and Kettle، نويسنده , , Jason G. and McMillan، نويسنده , , Caroline A. and Perkins، نويسنده , , Paula and Robins، نويسنده , , Peter and Smith، نويسنده , , Peter M. and Williams، نويسنده , , Emma J. and Wrigley، نويسنده , , Gail L.، نويسنده ,
Abstract :
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.
Keywords :
Buchwald–Hartwig amination , Regioselective substitution , 2-Chloro-N-phenylpyridin-4-amines , 4-Chloro-N-phenylpyridin-2-amines
