Central nervous system active compounds. IV. Synthesis of 3-aminobenzylphthalides

Abstract

Several 3-aminobenzylphthalides have been prepared by reactions of 3- (2-oxo-1-phenylpropyl)-phthalides with hydrazoic acid or by the Beckmann rearrangement. The corresponding reactions with 3-(2- oxoindanyl)phthalides showed limited success but led to a new synthesis of phthalide-isoquinoline alkaloids. Preliminary biological testing of some of these derivatives indicates that they only have weak central nervous system activity.