With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228779-96-1,3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide,as a common compound, the synthetic route is as follows.
To a solution of 3- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy) -4′- (2-phenylpyrrolidin-1-yl) -[1, 1′-biphenyl] -4-carboxylic acid (95 mg, 0.2 mmol) in dichloromethane (25 mL) were added HATU (114 mg, 0.3 mmol) and trimethylamine (0.2 mL). The mixture was stirred for 0.5 h at r.t. Then 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (126 mg, 0.4 mmol) was added. After stirred overnight at r.t, the reaction mixture was washed with water (10 mL), and the organic layers were dried over anhydrous Na 2SO 4, then concentrated in vacuum. The residue was further purified by prep-HPLC to give the desired compound. 1H NMR (400 MHz, DMSO-d 6) delta ppm: 12.16 (s, 1H), 11.68 (s, 1H), 8.57 (s, 1H), 8.54 (s, 1H), 8.03 (s, 1H), 7.80 (d, J = 8.6 Hz, 1H), 7.59-7.46 (m, 3H), 7.33-7.25 (m, 5H), 7.20-7.14 (m, 3H), 7.08 (d, J = 8.1Hz, 1H), 6.89 (s, 1H), 6.42 (d, J = 8.5 Hz, 2H), 6.37 (s, 1H), 4.78 (d, J = 7.4 Hz, 1H), 3.84 (d, J = 8.4 Hz, 2H), 3.68 (s, 1H), 3.31-3.20 (m, 3H), 2.37-2.34 (m, 1H), 1.94-1.80 (m, 4H), 1.60 (d, J = 12.0 Hz, 2H), 1.38-1.14 (m, 4H). MS (ESI, m/e) [M+1] + 773.3
1228779-96-1, As the paragraph descriping shows that 1228779-96-1 is playing an increasingly important role.
Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
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