| 主权项 |
1. A method of preparing a 2-arylindole compound, said method comprising:
providing a reaction medium comprising an N-heterocyclic carbene catalyst precursor compound, a base component and an o-aminobenzyl chloride compound of a formula wherein R1 is selected from H, halo, cyano, alkyl, haloalkyl and alkoxy moieties; R2 is selected from H and alkyl moieties; and R3 is selected from H and amino-protecting groups; introducing an arylaldehyde compound of a formula ArC(O)H to said reaction medium, wherein Ar is selected from aryl and heteroaryl moieties, where a said heteroatom is selected from S and N, said Ar moiety optionally substituted with one or more halo, cyano, alkyl, haloalkyl, alkoxy acetamido or acetamidoalkoxy groups and combinations thereof, to provide a benzylic ketone intermediate compound; and introducing an acid component to said reaction medium to promote intramolecular N—C bond formation and dehydration, to provide a 2-arylindole compound of a formula |
