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.
1228779-96-1, To a solution of 3- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy) -4′- (((S)-2-(2-cyclopropylphenyl) pyrrolidin-1-yl) methyl) -2′, 3′, 4′, 5′-tetrahydro- [1, 1′-biphenyl] -4-carboxylic acid (150 mg, 0.281 mmol) in DCM (20 mL) was added HATU (128 mg, 0.338 mmol), DMAP (34 mg, 0.281 mmol), TEA (141 mg, 1.405 mmol) and 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (106 mg, 0.338 mmol), the solution was stirred at r.t for 16h. The reaction solution was concentrated and purified by column chromatograph on silica gel (100-200 mesh, eluent: MeOH/DCM = 1/20) to give the crude product, which was purified by pre-TLC (MeOH/DCM = 1/15) to give the product as yellow solid. (60 mg, 25.7 %). 1H NMR (DMSO-d 6) delta ppm: 12.22 (s, 1H), 11.70 (s, 1H), 8.90-8.42 (m, 2H), 8.01 (s, 1H), 7.85-7.40 (m, 5H), 7.32-6.80 (m, 5H), 6.74-6.61 (m, 1H), 6.39 (s, 1H), 6.10-5.89 (m, 1H), 5.16-4.92 (m, 1H), 3.94-3.66 (m, 3H), 3.53-3.44 (m, 1H), 3.30-3.17 (m, 5H), 2.27-1.96 (m, 7H), 1.91-1.54 (m, 7H), 1.44-1.13 (m, 4H), 1.06-1.01 (m, 1H), 0.94-0.81 (m, 2H), 0.71-0.42 (m, 2H). [M+1] + 830.8.
The synthetic route of 1228779-96-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
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