- Access to 2-pyridinylamide and imidazopyridine from 2-fluoropyridine and amidine hydrochloride
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Under catalyst-free conditions, an efficient method to synthesize 2-pyridinylamides has been developed, and the protocol uses inexpensive and readily available 2-fluoropyridine and amidine derivatives as the starting materials. Simultaneously, the copper-catalysed approach to imidazopyridine derivatives has been established with high chemoselectivity and regiospecificity. The results suggest that the nitrogen-heterocycles containing iodide substituents can also be compatible for the reaction via the cascade Ullmann-type coupling, and the nucleophilic substitution reaction provides the target products in a one-pot manner.
- Chen, Lu,Huang, Shuo,Ji, Xiaoliang,Li, Jiaming,Li, Jian,Li, Yibiao,Liu, Jiasheng,Peng, Shiyong,Zhang, Kun
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supporting information
p. 9292 - 9299
(2020/12/03)
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- Improved Synthesis of 6-Chloro-5-methylpyridin-2-amine: A Key Intermediate for Making Lumacaftor
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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.
- Jiang, Xiangrui,Shen, Jingshan,Tian, Guanghui,Zhang, Junchi,Zhu, Fuqiang
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p. 1175 - 1179
(2020/07/06)
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- 4, 5-DIHYDRO-LH-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES
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Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
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Page/Page column 63-64
(2010/11/03)
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