以4-(4-氯丁酰基)-α,α-二甲基苯乙酸甲酯(5)为原料,与4-氰基哌啶(4)缩合,再与二苯甲酮(2)反应得到了2-[4-[4-[4-(羟基二苯甲基)-1-哌啶基]-1-氧代丁基]苯基]-2,2-二甲基乙酸甲酯(1),总收率约79%。该工艺反应条件温和,副反应少,易于操作,是一条适于工业化生产的合成路线。%2-[4-[4-[4-(Hydroxydiphenylmethyl) - 1 -piperidinyl]- 1 -oxobutyl]phenyl]-2,2 -dimethylaeetic acid methyl ester was synthesized from methyl 4-(4-chloro-l-oxobutyl)-α,α-dimethylphenyl acetate with piperidine- 4-carbonitrile to give methyl 2-(4-(4-(4-cyanopiperidin-l-yl)butanoyl)phenyl)-2-methylpropanoate,which was reacted with benzophenone and with an overall yield of 79%. This method is a suitable route for industrial manufacture with advantages of mild condition, few side reaction and easy operation.
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