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PROCESSES FOR PREPARATION OF N-PROTECTED- -AMINO ALCOHOLS AND N-PROTECTED- -AMINO EPOXIDES
PROCESSES FOR PREPARATION OF N-PROTECTED- -AMINO ALCOHOLS AND N-PROTECTED- -AMINO EPOXIDES
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机译:N-保护的氨基醇和N-保护的氨基化合物的制备方法
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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.
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