반응 #1725972

반응 방정식

diethyl phosphorocyanidate

7-benzyloxy-1,2-dihydro-3-naphthoic acid

1-(3,4,5-trimethoxybenzyl)piperazine dihydrochloride

triethylamine

→

1-(7-benzyloxy-1,2-dihydro-3-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride

수율 74.4%

용매

N,N-dimethylformamide

반응 조건

후처리

1. 1
   기타The reaction product is purified by silica gel column chromatography (hexane:acetone=1:1-1:2)
2. 2
   workup.ADDITIONconverted to the hydrochloride in a mixture of ethyl acetate and ethyl ether

실험 절차

Using 7-benzyloxy-1,2-dihydro-3-naphthoic acid (0.4 g), 1-(3,4,5-trimethoxybenzyl)piperazine dihydrochloride (0.76 g), triethylamine (0.6 g), N,N-dimethylformamide (10 ml) and diethyl phosphorocyanidate (0.75 ml), an amidation as that described in Example 6 is carried out. The reaction product is purified by silica gel column chromatography (hexane:acetone=1:1-1:2) and converted to the hydrochloride in a mixture of ethyl acetate and ethyl ether to yield 1-(7-benzyloxy-1,2-dihydro-3-naphthoyl)-4-(3,4,5-trimethoxybenzyl)piperazine hydrochloride (0.6 g) as colorless crystals, m.p. 196°-199° C. (decomp.).

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