在水中利用 Micelle Enabled Buchwald-Hartwig Amination 与 Bening by Design 表面活性剂 TPGS-750-M 合成 JAK 抑制剂 4-((2-氯苯基)氨基)-6-((6-甲基吡啶-2-基)氨基)烟酰胺

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY Accounts of Chemical Research Pub Date : 2024-08-11 DOI:10.1002/hlca.202400094

Hao Jiang, Bin Wu, Dominik Rufle, Liping Wang, Min Shi, Michael Parmentier, Fabrice Gallou

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引用次数: 0

摘要

本研究介绍了一种高效、可扩展的布赫瓦尔德-哈特维格胺化法，用于合成候选原料药 4-((2-氯苯基)氨基)-6-((6-甲基吡啶-2-基)氨基)烟酰胺，作为一种 JAK 抑制剂。该工艺使用水和一种水溶性助溶剂进行开发。设计中使用的良性表面活性剂 TPGS-750-M 促进了目标化合物的可靠制备，不仅产率高，反应曲线也得到了改善，而且操作简便。

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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Micelle Enabled Buchwald-Hartwig Amination in Water with the Bening by Design Surfactant TPGS-750-M for the Synthesis of the JAK Inhibitor 4-((2-Chlorophenyl)amino)-6-((6-methylpyridin-2-yl)amino)nicotinamide

An efficient and scalable Buchwald-Hartwig amination towards the synthesis of the API candidate 4-((2-Chlorophenyl)amino)-6-((6-methylpyridin-2-yl)amino)nicotinamide as a JAK inhibitor was described. The process was developed using water and a water-miscible co-solvent. It was facilitated by the benign by design surfactant TPGS-750-M, that promoted the robust and reliable preparation of our target compound in high yields, with improved reaction profile and via an operationally simple protocol.

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.

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