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首页> 外文期刊>RSC Advances >Enantioselective synthesis of 1,2,5,6-tetrahydropyridines (THPs) via proline-catalyzed direct Mannich-cyclization/domino oxidation–reduction sequence: application for medicinally important N-heterocycles
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Enantioselective synthesis of 1,2,5,6-tetrahydropyridines (THPs) via proline-catalyzed direct Mannich-cyclization/domino oxidation–reduction sequence: application for medicinally important N-heterocycles

机译：通过脯氨酸催化的直接曼尼希 - 环化/多米诺氧化还原序列对1,2,5,6-四氢吡啶（THPS）的映选择性合成：用于药用重要的N-杂环

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摘要

An enantioselective multi-component synthesis of 1,2,5,6-tetrahydropyridines (THPs) has been developed through a one-pot domino-process. This transformation proceeds through proline-catalyzed direct Mannich reaction-cyclization of glutaraldehyde with in situ generated imines, followed by site-selective oxidation–reduction sequence under mild conditions. Chiral 1,2,5,6-THPs are obtained in good to high yields (up to 80%) and with the excellent enantioselectivity (up to 98?:?2 er). The usefulness of this operationally simple method is also shown to synthesize other medicinally important nitrogen-heterocycles.
机译：通过单锅Domino-Procine开发了1,2,5,6-四氢吡啶（THP）的对映选择性的多组分合成。该转化通过脯氨酸催化的直接曼尼希反应环化与原位产生的亚胺，然后在温和条件下进行位点选择性氧化还原序列。高产率（高达80％）获得手性1,2,5,6-6PP，并且具有出色的对映选择性（高达98？：2ER）。该操作简单方法的有用性也被证明是合成其他药用重要的氮杂杂环。

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