Reference of 612511-81-6, These common heterocyclic compound, 612511-81-6, name is (1-Methyl-1H-pyrazol-3-yl)methanamine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To 4-fluoro-N-methyl-3-nitrobenzamide (350 mg, 1 .766 mmol) in DMF (5 mL) were added (1 -methyl-1 H-pyrazol-3-yl)methanamine (206 mg, 1 .855 mmol) and K2C03 (317 mg, 2.296 mmol), and the reaction mixture was stirred at room temperature overnight. The reaction was then quenched with water (10 mL), and the resulting solid was isolated by filtration, washed with water, and dried in vacuum oven for 4 hours to afford N-methyl-4-(((1 -methyl- 1 H-pyrazol-3-yl)methyl)amino)-3-nitrobenzamide (390 mg) as an orange color solid. LC-MS (ES) m/z = 290 [M+H]+. NMR (400 MHz, DMSO-d6): delta 2.76 (d, J = 4.3 Hz, 3H), 3.81 (s, 3 ), 4.57 (d, J = 5.3 Hz, 2H), 6.19 (d, J = 2.0 Hz, 1 H), 7.15 (d, J = 9.1 Hz, 1 H), 7.64 (d, J = 2.3 Hz, 1 H), 7.96 (dd, J = 9.0, 2.2 Hz, 1 H), 8.46 (d, J = 4.8 Hz, 1 H), 8.63 (d, J = 2.3 Hz, 1 H), 8.77 (t, J = 5.6 Hz, 1 H).
The synthetic route of 612511-81-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; MEDINA, Jesus Raul; TIAN, Xinrong; NG DI MARCO, Christina; GRAYBILL, Todd L.; HEERDING, Dirk A.; LI, William Hoi Hong; MANGATT, Biju; MARTYR, Cuthbert D.; RIVERO, Raphael Anthony; (570 pag.)WO2019/49061; (2019); A1;,
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