【药物名称】RS-86
化学结构式(Chemical Structure):
参考文献No.42002
标题:Improvements in or relating to Spiropiperidyl-Succinimide Derivatives
作者:Br黶chweiler, C.; Schereier, E.; S黣s, R.; Winkler, H.
来源:CH 411895; CH 449628; GB 1041015
合成路线图解说明:

The condensation of 1-methyl-4-piperidone (I) with ethyl cyanoacetate (II) in refluxing acetic acid gives ethyl (1-methyl-4-piperidylidene)cyanoacetate (III), which by reaction with KCN in ethanol is converted to ethyl (1-methyl-4-cyano-4-piperidyl)cyanoacetate (IV). The decarboxylative hydrolysis of (IV) with refluxing aqueous HCl affords (1-methyl-4-carboxy-4-piperidyl)acetic acid (V), which is esterified with ethanol - HCl to its diethyl ester (VI). Finally, this compound is treated with ethylamine at 200 C.

参考文献No.65133
标题:RS-86
作者:Ghose, K.
来源:Drugs Fut 1986,11(4),276
合成路线图解说明:

The condensation of 1-methyl-4-piperidone (I) with ethyl cyanoacetate (II) in refluxing acetic acid gives ethyl (1-methyl-4-piperidylidene)cyanoacetate (III), which by reaction with KCN in ethanol is converted to ethyl (1-methyl-4-cyano-4-piperidyl)cyanoacetate (IV). The decarboxylative hydrolysis of (IV) with refluxing aqueous HCl affords (1-methyl-4-carboxy-4-piperidyl)acetic acid (V), which is esterified with ethanol - HCl to its diethyl ester (VI). Finally, this compound is treated with ethylamine at 200 C.

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