Analyzing the synthesis route of 1211523-71-5

At the same time, in my other blogs, there are other synthetic methods of this type of compound,1211523-71-5, 2-(2-Bromopyridin-3-yl)acetonitrile, and friends who are interested can also refer to it.

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.1211523-71-5, name is 2-(2-Bromopyridin-3-yl)acetonitrile, molecular formula is C7H5BrN2, molecular weight is 197.03, as common compound, the synthetic route is as follows.SDS of cas: 1211523-71-5

To a 0C solution of 2-(2-bromopyridin-3-yl)acetonitrile (2.21 g, 11.21 mmol) inDMF (20 mL) was added NaH (60% dispersion in mineral oil, 1.12 g, 28.03 mmol) in portions. The resulting mixture was warmed to 60 C and stirred for 1.5 h. Tert-butylbis(2-chloroethyl)carbamate (3.26 g, 13.46 mmol) was added to the mixture and stirred for 2 h at 60 C. After cooling to RT, the reaction mixture was quenched with brine (50 mL), extracted with EA (3 x 100 mL). The combined organic layers were washed with brine (3 x 80 mL), dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure. The residue was purified by silica chromatography (eluting with EA: Hex = 1: 3, v/v) to give tert-butyl4-(2-bromopyridin-3-yl)-4-cyanopiperidine-1-carboxylate (1.56 g). MS: m/z 366 (M+H) .

At the same time, in my other blogs, there are other synthetic methods of this type of compound,1211523-71-5, 2-(2-Bromopyridin-3-yl)acetonitrile, and friends who are interested can also refer to it.

Reference:
Patent; JACOBIO PHARMACEUTICALS CO., LTD.; JACOBIO-ALPHA PHARMACEUTICALS CO., LTD.; MA, Cunbo; GAO, Panliang; HU, Shaojing; XU, Zilong; HAN, Huifeng; WU, Xinping; KANG, Di; LONG, Wei; (202 pag.)WO2018/172984; (2018); A1;,
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