In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 4331-28-6, name is 1H-Pyrazol-4-amine hydrochloride belongs to pyrazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below. Computed Properties of C3H6ClN3
2-(Methoxy(phenyl)methyl)-6-(methylcarbamoyl)isonicotinic acid (150 mg, 0.50 mmol) was added to a dry flask. DMF (2 mL) was added, followed by HATU (228 mg, 0.60 mmol) and 1H-pyrazol-4-amine, hydrochloride (59.7 mg, 0.50 mmol). The reaction was stirred for 2 mm and then DIPEA (0.262 mL,1.498 mmol) was added. The reaction was stirred at rt for 30 mm. The reaction mixture was added directly to 3 x LCMS vials, diluting with DMS0/Me0H and purified by 3 x MDAP (High pH). Theappropriate fractions were concentrated in vacuoto afford the desired product as a yellow solid – (+1- )-6-(methoxy(phenyl)methyl)-N2-methyl-N4-( 1 H-pyrazol-4-yl)pyridine-2,4-dicarboxamide (100 mg, 0.27 mmol, 55 % yield)LCMS (2 mm Formic): Rt = 0.82 mi [MH]+ = 366.3.1H NMR (400 MHz, DMS0-d6) O ppm 12.69 (br. s., 1 H) 10.92 (5, 1 H), 8.67 (q, J=4.8 Hz, 1H), 8.45 (d, J=1.7 Hz, 1 H), 8.17 (d, J=1.5 Hz, 1 H), 8.04 (br. 5., 1 H), 7.72 (br. 5., 1 H), 7.51 (d, J=7.1 Hz, 2 H), 7.36 (t, J=7.5 Hz, 2 H), 7.24 – 7.31 (m, 1 H), 5.52 (5, 1 H), 3.39 (5, 3 H), 2.88 (d, J=4.9 Hz, 3 H)
The synthetic route of 4331-28-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (N.2) LIMITED; ATKINSON, Stephen John; DEMONT, Emmanuel Hubert; HARRISON, Lee Andrew; LEVERNIER, Etienne; PRESTON, Alexander G; SEAL, Jonathan, Thomas; WALL, Ian David; WATSON, Robert J; WOOLVEN, James Michael; (0 pag.)WO2018/158210; (2018); A1;,
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