RS-86
2-乙基-8-甲基-2,8-二氮杂螺[4.5]-1,3-癸二酮Chemical Name: 2-Ethyl-8-methyl-2,8-diazaspiro[4.5]decane-1,3-dione hydrobromide; Spiro(1-methyl-4-piperidyl)-(N-ethylsuccinimide) hydrobromide
CAS No. 3576-73-6 (free base), 51382-46-8 (fumarate)
项目整合开发状态: Phase II
项目研究机构: Novartis (Originator)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Improvements in or relating to Spiropiperidyl-Succinimide Derivatives
文献作者:Br黶chweiler,C.; Schereier,E.; S黣s,R.; Winkler,H.
参考来源:CH 411895; CH 449628; GB 1041015
📄 详细内容
合成路线: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.
参考文献标题:RS-86
文献作者:Ghose,K.
参考来源:Drugs Fut 1986,11(4),276
产品链接: CAS No. 3576-73-6››