反应详情

Using 6,7-dimethoxy-2-naphthoic acid (0.7 g), 1-(3,4,5-trimethoxybenzyl)piperazine dihydrochloride (1.1 g), triethylamine (1.25 g), N,N-dimethylformamide (20 ml) and diethyl phosphorocyanidate (1 ml), an amidation as that described in Example 6 is carried out. The product is purified by silica gel column chromatography (hexane:acetone=2:3) and converted to the hydrochloride in ethyl acetate to give 1-(6,7-dimethoxy-2-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride (1.25 g) as colorless crystals, m.p. 235°-240° C. (decomp.).

1. customThe product is purified by silica gel column chromatography (hexane:acetone=2:3)