三光气法合成盐酸罗哌卡因

Synthesis of Ropivacaine Hydrochloride by Triphosgene

以三光气为酰氯化剂,2-哌啶甲酸经酰氯化,酰胺化制得1-N-(2,6-二甲基苯基)-2-哌啶甲酰胺(2),收率50.1%(以2-哌啶甲酸计)。以DMF为溶剂,2经丙基化反应合成了盐酸罗哌卡因(1),收率54%。1和2的结构经1H NMR表征。

Ropivacaine hydrochloride in 54% yield was synthesized from N-（2,6-dimethylphenyl）-piperidine-2-carboxamide）, which was obtained in 50. 1% yield from 2-pipecolic acid by chlorination using triphosgene as an acyl chlorination agent and amidation. The structures were confirmed by 1^H NMR.