Department of Process Research, Merck Frosst Centre for Therapeutic Research, 16711 Autoroute Transcanadienne, Kirkland, Quebec, Canada H9H 3L1.
Org Lett. 2010 Sep 3;12(17):3772-5. doi: 10.1021/ol101406k.
A practical procedure for the enzymatic resolution of 2-alkyl-2-aryl-disubstituted epoxides using the Codex HHDH P2E2 enzyme and sodium azide is reported. This method allowed the synthesis of novel regio- and enantioselective 1-azido-2-arylpropan-2-ols in excellent yields. Furthermore, these intermediates were used for the preparation of enantiomerically enriched amino alcohols and aziridines containing a tertiary center.
本文报道了使用 Codex HHDH P2E2 酶和叠氮化钠对 2-烷基-2-芳基取代环氧化合物进行酶促拆分的实用方法。该方法能够以优异的收率合成新型区域和对映选择性的 1-叠氮基-2-芳基-2-丙醇。此外，这些中间体还可用于制备含有三级中心的对映体富集的氨基醇和氮丙啶。
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