益母草碱中间体N,N-二叔丁氧基羰基-胍基丁醇的合成  

Synthesis of Leonurine Intermediates,N,N'-di(tert-buto-xycarbony-l)guanidinylbutanol

作　　者：王锦芝[1] 何小英[1] 张鲁勉[1] 叶婷君[1] 郑锦鸿[1] 

机构地区：[1]汕头大学医学院化学教研室,广东汕头515041

出　　处：《汕头大学医学院学报》2011年第4期211-213,共3页Journal of Shantou University Medical College

摘　　要：目的:优化益母草碱中间体N,N-二叔丁氧基羰基-胍基丁醇的合成方法。方法:用S-烷基化异硫脲法和Mukaiyama法分别进行中间体的合成,并进行比较。结果:N,N-二叔丁氧基羰基-S-甲基异硫脲在Mukaiyama试剂和三乙胺条件下,与4-氨基-1-丁醇反应可得到双保护的中间体;且反应条件温和,总收率68.5%,产品纯度好,其结构经熔点、质谱和核磁共振谱确定。结论:Mukaiyama试剂法合成中间体,收率高,纯度好。Objective：To optimiz the synthetic method of the leonurine intermediate,N,N＇-di（tert-buto-xycarbonyl）-guanidinylbutanol.Methods：The intermediate was synthesized by S-alkyliso-thioureas and Mukaiyama＇s reagents methods respectively and compared.Results：4-amino-1-butanol reacted with N,N＇-di（tertbutoxycarbonyl）-S-methylisothiourea in the presence of Mukaiyama＇s reagent and triethylamine to receive the intermediate.The overall yield of product was 68.5%,The structure of the product was identified by m.p.,MS and 1H-NMR.Conclusion：The intermediate is obtained with higher yield and better purity by Mukaiyama＇s reagent.

关 键 词：N N-二叔丁氧基羰基-胍基丁醇 合成 

分 类 号：O622.6[理学—有机化学]