简单的一锅衍生化硝基吡啶方案:获得3-乙酰氨基吡啶-2-基4-甲基苯磺酸衍生物

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2019-01-01 DOI:10.1515/hc-2019-0017

Ling‐Zhi Lin, Xiaoguang Chen, Junhao Zhao, Suitao Lin, Guojian Ma, Xiaojian Liao, Pengju Feng

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引用次数: 1

摘要

摘要:本文揭示了一种高效的一锅法将易于获取的3-硝基吡啶转化为3-乙酰氨基吡啶-2-酰基4-甲基苯磺酸盐衍生物，这是许多药物分子的核心结构。该策略通过在一个锅中逐步加入不同的反应物，成功地将三步反应结合在一起。该反应具有良好的官能团耐受性和区域选择性。结构多样化的3-硝基吡啶可以在3.5 h内快速衍生出各种功能的2-O,3- n -吡啶，便于进一步的细化。这种转变符合克尺度的综合。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Facile One-pot Protocol of Derivatization Nitropyridines: Access to 3-Acetamidopyridin-2-yl 4-methylbenzenesulfonate Derivatives

Abstract This paper discloses an efficient one-pot protocol to convert easily accessible 3-nitropyridines to 3-acetamidopyridin-2-yl 4-methylbenzenesulfonate derivatives which are core structures of many pharmaceutical molecules. The strategy successfully combined a three-step reaction in one pot via progressively adding different reactants at rt. The reaction displays good functional group tolerance and regioselectivity. Structurally diversified 3-nitropyridine could be time-efficiently (3.5 h) derivatized to various functional 2-O,3-N-pyridines which are apt for further elaborations. The transformation was amenable to gram-scale synthesis.

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.