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.573762-62-6, name is 5-Amino-3-(trifluoromethyl)picolinonitrile, molecular formula is C7H4F3N3, molecular weight is 187.12, as common compound, the synthetic route is as follows.HPLC of Formula: C7H4F3N3
Add 99mg (0.25mmol, 1.0eq) JD1001-002-22 to a 25mL round bottom flask under nitrogen protection., 3.2 mL THF, 63 mg (0.75 mmol, 3.0 eq) NaHCO3, 140 mg (0.75 mmol, 3.0 eq)5-Amino-3-trifluoromethyl-2-cyanopyridine, stirred at 60 C for 3 hours with heating, TLC detection reaction was completed (developing agent: PE: EA = 1:1), added5 ml of water was quenched and EA was extracted to give an organic phase.Concentrating the organic phase to give a solid,Separated by HPLC (CH3CN/H2O=60:40)purification,After lyophilization, about 16 mg of product JD1001-2139 is obtained.The yield was 13%.
At the same time, in my other blogs, there are other synthetic methods of this type of compound,573762-62-6, 5-Amino-3-(trifluoromethyl)picolinonitrile, and friends who are interested can also refer to it.
Reference:
Patent; Kunming Jida Pharmaceutical Co., Ltd.; Xiao Xuzhi; Zhang Poyong; Lu Faguan; Wang Zhipeng; Chen Mengran; Guo Kun; Zhou Rui; Zhang Yun; (28 pag.)CN109593061; (2019); A;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem