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Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2020-04-24 , DOI: 10.1021/acs.oprd.9b00556
Junchi Zhang 1, 2 , Fuqiang Zhu 3 , Guanghui Tian 3 , Xiangrui Jiang 1, 2 , Jingshan Shen 1, 2
Affiliation  

A safe and efficient synthesis of 6-chloro-5-methylpyridin-2-amine, a key intermediate for lumacaftor, is described, which avoids the utilization of peroxide. In this four-step sequence, starting from 2-amino-6-chloropyridine, the crucial 5-position methylation was achieved via a Suzuki-Miyaura cross-coupling reaction. By adopting this synthetic route, 6-chloro-5-methylpyridin-2-amine was produced on a hectogram scale with 62.4% overall yield and 99.49% purity.

中文翻译:

改进的6-氯-5-甲基吡啶-2-胺的合成:制备鲁马卡托的关键中间体

描述了一种安全有效的合成方法6-氯-5-甲基吡啶-2-胺,它是鲁马卡托的关键中间体,它避免了过氧化物的利用。在这四个步骤中,从2-氨基-6-氯吡啶开始,关键的5位甲基化是通过Suzuki-Miyaura交叉偶联反应实现的。通过采用这种合成途径,以百克规模生产了6-氯-5-甲基吡啶-2-胺,总产率为62.4%,纯度为99.49%。
更新日期:2020-06-19
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