摘要
4-哌啶甲酸在三甲基氯硅烷作用下酯化、与溴乙酸乙酯进行N-烷基化反应制得1-乙氧甲酰基甲基哌啶-4-甲酸乙酯,再经Dieckmann反应制得药物中间体3-奎宁环酮,总收率约70%。
3-Quinuclidone, the key intermediate for some drugs, was prepared from piperidine-4-carboxylic acid by esterification with alcohol in the presence of chlorotrimethylsilane, N-alkylation with ethyl bromoacetate in ethanol to give ethyl 1-carbethoxymethylpiperidine-4-carboxylate followed by Dieckmann reaction with an overall yield of about 70 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2007年第4期260-261,共2页
Chinese Journal of Pharmaceuticals
关键词
3-奎宁环酮
中间体
制备
3-quinuclidone
intermediate
preparation
