Catalytic C-H bond silylation of aromatic heterocycles

摘要: This protocol describes a method for the direct silylation of carbon-hydrogen (C-H) bond aromatic heterocycles using inexpensive and abundant potassium tert-butoxide (KOt-Bu) as catalyst. catalytic cross-dehydrogenative coupling simple hydrosilanes various electron-rich enables synthesis valuable silylated heteroarenes. The products thus obtained can be used versatile intermediates, which facilitate divergent pharmaceutically relevant compound libraries from single Si-containing building block. Moreover, variety complex motifs, such those produced by this protocol, are being actively investigated next-generation therapeutic agents, because they have improved pharmacokinetic properties compared with original all-carbon drug molecules. Current competing methods C-H tend to incompatible functionalities, Lewis-basic heterocycles, that often found in pharmaceutical substances; leaves de novo principal strategy preparation target sila-drug analog. limited scope hydrosilane used, restricts breadth silicon-containing small molecules accessed. approach outlined chemoselective regioselective late-stage including drugs derivatives, broad array absence precious metal catalysts, stoichiometric reagents, sacrificial hydrogen acceptors or high temperatures. H2 is only by-product generated. procedure normally requires 48-75 h completed.