HYPERVALENT IODINE MEDIATED ONE-POT C-H FUNCTIONALIZATION AT 2α- OR 3α-POSITION OF INDOLE DERIVATIVES

摘要

The one-pot 2α- and 3α-functionalization of 2,3-disubstituted indoles using a hypervalent iodine reagent has been developed. The substitution at the 2a-position of indoles took place using phenyliodinebis(trifluoroacetate) with oxygen and carbon nucleophiles in moderate yields. The combination of iodosobenzene and trimethylsilyl azide afforded 3α-azide derivatives preferentially. The latter reaction was applied to other 2,3-disubstituted indoles.