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Processes for preparation of N-protected-β-amino alcohols and N-protected-β-amino epoxides

机译:N-保护的β-氨基醇和N-保护的β-氨基环氧化物的制备方法

摘要

Herein are disclosed a process for increasing in purity, or purifying, an N-protected-β-aminoalcohol which process comprises (i) adding water to a polar organic solvent in which an N-protected-β-aminoalcohol such as a (2R,3S)- or (2S,3R)-3-tert-butoxycarbonylamino-1-halo-2-hydroxy-4-phenylbutane or the like, or (ii) crystallizing such an N-protected-β-aminoalcohol from a diol or a diol-based mixed solvent, and a process for producing the corresponding N-protected-β-aminoepoxide which process comprises treating, with a base, the thus purity-enhanced N-protected-β-aminoalcohol. Such N-protected-β-aminoalcohols and N-protected-β-aminoepoxides are both useful as synthetic intermediates for medicine compounds, such as, e.g., HIV protease inhibitor and the like.
机译:本文公开了一种提高纯度或纯化N-保护的β-氨基醇的方法,该方法包括(i)将水加到极性有机溶剂中,其中N保护的β-氨基醇如(2R, 3S)-或(2S,3R)-3-叔丁氧基羰基氨基-1-卤-2-羟基-4-苯基丁烷或类似物,或(ii)从二醇或苯甲酸酯中结晶这种N-保护的β-氨基醇。二醇基混合溶剂,以及制备相应的N-保护的-β-氨基环氧化物的方法,该方法包括用碱处理如此纯度提高的N-保护的-β-氨基醇。这样的N-保护的β-氨基醇和N-保护的β-氨基环氧化物均可用作药物化合物的合成中间体,例如HIV蛋白酶抑制剂等。

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