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 1.5 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Helvetica Chimica Acta 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

Helvetica Chimica Acta 化学-化学综合

CiteScore

3.00

自引率

0.00%

发文量

审稿时长

2.3 months

期刊介绍： Helvetica Chimica Acta, founded by the Swiss Chemical Society in 1917, is a monthly multidisciplinary journal dedicated to the dissemination of knowledge in all disciplines of chemistry (organic, inorganic, physical, technical, theoretical and analytical chemistry) as well as research at the interface with other sciences, where molecular aspects are key to the findings. Helvetica Chimica Acta is committed to the publication of original, high quality papers at the frontier of scientific research. All contributions will be peer reviewed with the highest possible standards and published within 3 months of receipt, with no restriction on the length of the papers and in full color.