Patent ID: 8212047
Filing Date: 2012-07-03
Classification: C07D

Abstract:
1. A method for synthesizing a functionalized pyridyl-amine product comprising the following steps: (a) providing a di-substituted pyridine reactant having the following formula: (b) selectively activating one of the X (c) reacting the mono-metallated, halo-substituted pyridine intermediate with one or more other reactants under conditions sufficient to form a halo-substituted pyridinyl aldehyde intermediate; (d) arylating the halo-substituted pyridinyl aldehyde intermediate by contacting it with an optionally substituted aryl-dihydroxyborane under conditions sufficient to form an (optionally substituted aryl)-substituted pyridinyl aldehyde intermediate; and (e) aminating the (optionally substituted aryl)-substituted pyridinyl aldehyde intermediate by contacting it with one or more other reactants under conditions sufficient to form the functionalized pyridyl-amine product.