Related Products of 52378-63-9, 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.52378-63-9, name is (3-Aminopyridin-2-yl)methanol, molecular formula is C6H8N2O, molecular weight is 124.14, as common compound, the synthetic route is as follows.
Example 59 5-Fluoro-N-(3-hydroxymethyl-pyridin-2-yl)-2-(3-methylsulfanyl-phenoxy)-nicotinamide 2-Hydroxymethyl-3-aminopyridine (89 mg, 0.716 mmol) and triethylamine (200 l, 2.14 mmol) were dissolved in dimethylformamide (1 ml) under nitrogen at room temperature and a solution of 5-Fluoro-2-(3-methylsulfanyl-phenoxy)-nicotinic acid (200 mg, 0.716 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (151 mg, 0.788 mmol) and 1-hydroxybenzotriazole (106 mg, 0.788 mmol) in dimethylformamide (5 ml) and the reaction was stirred at room temperature for 18 h. The reaction mixture was concentrated under reduced pressure, and the residue was purified by flash column chromatography on silica gel eluding with a solvent gradient of dichloromethane:methanol:concentrated aqueous ammonia (97.5:2.5:0.25 changing to 95:5:0.5, by volume) and the product was crystallized from diisopropyl ether (5 ml) to give 5-Fluoro-N-(3-hydroxymethyl-pyridin-2-yl)-2-(3-methylsulfanyl-phenoxy)-nicotinamide (127 mg) as an off-white solid. 1H NMR (400 MHz, CDCl3): delta=8.14-8.16 (1H, d), 8.06-8,08 (1H, dd), 8.02-8.04 (1H, dd), 7.50-7.54 (1H, d), 7.28-7.32 (1H, t), 7.10-7.14 (1H, d), 6.97 (1H, s), 6.84-6.88 (1H, d), 6.46-6.50 (1H, d), 5.33 (2H, s), 4.89 (2H, brs), 2.45 (3H, s) ppm. LRMS (electrospray): m/z [M+H]+ 386, [M+Na]+ 408, [2M+Na]+ 793, [M-H]+ 384. Anal. Found C, 58.83; H, 4.16; N, 10.73. C19H16FN3O3S requires C, 59.21; H, 4.19; N, 10.90%.
Statistics shows that 52378-63-9 is playing an increasingly important role. we look forward to future research findings about (3-Aminopyridin-2-yl)methanol.
Reference:
Patent; Pfizer Inc; US2005/20587; (2005); A1;,
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