Direct synthesis of H-aryl and H-heteroarylphosphinic esters via palladium-catalyzed cross-coupling of alkylphosphinates

Aryl, heteroaryl, and benzylic electrophiles can be coupled to in situ-generated alkylphosphinates (ROP(O)H 2 ) in moderate to good yields using palladium catalysis. For the first time, electrophiles other than simple aryl iodides can be employed in an experimentally straightforward, one-pot reaction. The direct formation of H-phosphinic esters avoids the separate esterification of H-phosphinic (phosphonous) acids and is particularly useful in the case of nitrogen-containing heteroaromatics. The reaction significantly expands the scope of related palladium-catalyzed phosphorus-carbon bond-forming reactions.