Patent ID: 6133452
Filing Date: 2000-10-17
Classification: C07D

Abstract:
A process of preparing compounds of Formula Ia: ##STR26## wherein: R.sub.1 is ##STR27## and R.sub.2 is ##STR28## which comprises, reacting an indole-3-acetamide of the formula ##STR29## with an indolyl-3-glyoxyl reagent of the formula ##STR30## wherein: R.sub.3 is I, Cl, Br, or OR.sub.4 ;R.sub.4 is C.sub.1 -C.sub.4 alkyl;R.sub.7 and R.sub.7 ' are independently hydrogen, alkyl, haloalkyl, arylalkyl, C.sub.1 -C.sub.4 alkoxy, optionally protected hydroxyalkyl, optionally protected aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, trialkylaminoalkyl, or COO(C.sub.1 -C.sub.4 alkyl);R.sub.8 is independently hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, (CH.sub.2).sub.m, hydroxy, acetyl, carboxy, halo, haloalkyl, nitro, and (CH.sub.2)mNR.sub.5 R.sub.6 ; wherein m is independently 0, 1, 2, or 3; and R.sub.5 and R.sub.6 are independently hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, or benzyl;in the presence of a base sufficiently strong to deprotonate the amide and methylene at the C-3 position of the indolyl-3-acetamide.