卡比多巴的合成  

Synthesis of Carbidopa

作　　者：钟为慧[1] 江灵波[1] 陈霄[1] 李振华[1] 

机构地区：[1]浙江工业大学药学院,浙江杭州310014

出　　处：《中国医药工业杂志》2008年第10期730-732,共3页Chinese Journal of Pharmaceuticals

基　　金：浙江省科技计划项目(2005C21042)

摘　　要：L-α-(3,4-二甲氧基苄基)-α-氨基丙腈盐酸盐经水解、与尿素在碱性介质中缩合制得L-α-(3,4-二甲氧基苄基)-α-脲基丙酸,再经Hofmann重排、48%氢溴酸脱甲基制得卡比多巴,总收率约25%。Carbidopa was synthesized from L-α-（3,4-dimethoxybenzyl）-α-aminopropionitrile hydrochloride via hydrolysis with concentrated hydrochloric acid and condensation with urea in the presence of base to afford the key intermediate L-α-（3,4-dimethoxybenzyl）-α-ureidopropanoic acid, which was subjected to Hofmann rearrangement and then deprotection by 48 % hydrobromic acid with an overall yield of about 25 %.

关 键 词：卡比多巴 帕金森病 合成 

分 类 号：R971.5[医药卫生—药品]