Electric Literature of 7341-96-0, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 7341-96-0 as follows.
To a cooled (0 C), clear, yellow solution of 4-chloro-3-fluoro-2-(6- methoxypyrimidin-4-yl)aniline (1 g, 3.94 mmol) in ACN (56.3 ml) was added isoamylnitrite (0.79 ml, 5.91 mmol), followed by the dropwise addition of TMSN3 (0.79 ml, 5.91 mmol). After 10 mm, the cold bath was removed, and the reaction was allowed to warm to rt and stirred at rt for lh. Next, propiolamide (0.8 17 g, 11.83 mmol) andCu20 (0.05 6 g, 0.3 94 mmol) were added. After 1 h, the yellow cloudy reaction was diluted with EtOAc, and washed with sat NH4C1, brine, dried over MgSO4, filtered and concentrated to give a yellow solid. DCM (10 ml) was added and the resulting mixture was sonicated. The suspension was filtered and the solid was air-dried. A yellow solid obtained as 1 -(4-chloro-3 -fluoro-2-(6-methoxypyrimidin-4-yl)phenyl)- 1 H- 1,2,3 -triazole25 4-carboxamide (1.003 g, 73.0% yield). MS(ESI) m/z: 349.0 (M+H).
According to the analysis of related databases, 7341-96-0, the application of this compound in the production field has become more and more popular.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; CORTE, James R.; DE LUCCA, Indawati; FANG, Tianan; YANG, Wu; WANG, Yufeng; DILGER, Andrew K.; PABBISETTY, Kumar Balashanmuga; EWING, William R.; ZHU, Yeheng; WEXLER, Ruth R.; PINTO, Donald J. P.; ORWAT, Michael J.; SMITH, Leon M. II; WO2015/116886; (2015); A1;,
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