摘要
(R)-3-氨基丁醇(1)是合成抗HIV/AIDS新药度鲁特韦的重要中间体。以(R)-(+)-α-苯乙胺(2)和乙酰乙酸乙酯(3)为原料,经过缩合、烯胺还原、差向异构体分离、酯还原和脱保护,得到纯品(R)-3-氨基丁醇,总收率达到39.3%。产品经过核磁氢谱和核磁碳谱表征。该路线能有效减少副产物。
(R)-3-amino-1-butanol,an important intermediate of dolutegravir,was prepared in a total yield of 39.3% from(R)-α-phenylethylamine and ethyl acetoacetate by sequential condensation,enamine reduction,separation of lepimers and deprotection.The structures of all the intermediates and the final product were confirmed by ~1H NMR and ~(13)C NMR.This synthetic route could effectively reduce the formation of by-products.
引文
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