(2S,3R)-2-苄氧羰基胺基-3,4-二羟基丁酰胺的合成

Synthesis of (2S,3R)-2-(benzyloxycarbonyl)amino-3,4-dihydroxybutyramide

目的研究卡芦莫南重要中间体的合成工艺并对其工艺进行改进。方法采用乙酰氯作为脱水剂形成异丙叉保护基及Gabriel反应合成伯胺的方法,避免了氯化氢气体的通入及叠氮化反应过程。结果经过改进的合成路线,九步反应合成目标化合物(Ⅱ),总收率与文献值接近。结论经过改进的此路线与原路线相比具有安全性高、原料易得、成本更低的优点。

Objective To study the synthesis of important intermediates of carumonam and improve their technology. Methods Acetyl chloride, as a dehydrating agent, was used for isopropylidene protecting groups. Gabriel synthesis of primary amine, avoided the use of hydrogen chloride gas and reaction of azide. Results The compound （II） was synthesized by nine-step reaction, and total yield was close to literature values. Conclusion This improved route, compared with the original line, raise the utilization rate, so it is more safe, lower cost, and more suitable for large-scale industrial production.