Electric Literature of 58483-98-0, 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.58483-98-0, name is 2-Amino-5-bromonicotinamide, molecular formula is C6H6BrN3O, molecular weight is 216.04, as common compound, the synthetic route is as follows.
To a mixture of 2-amino-5-bromonicotinamide (200 mg, 0.93 mmol), thiophene-2- carbaldehyde (125 mg, 1.11 mmol) in MeOH (15 mL) was added 4-methylbenzenesulfonic acid (16mg, 0.09 mmol). The mixture was stirred at 60C overnight. Then the resulting solid was filtered to give the product of 6-bromo-2-(thiophen-2-yl)-2,3 -dihydropyrido [2 ,3-d]pyrimidin-4( 1 H)-one (180 mg, yield: 63%), which was used for the next step without further purification. ?H NMR (DMSO-d6, 400 MHz) 8.93 (d, J= 2.4 Hz, 1H), 8.42 (s, 1H), 8.28 (d, J= 2.4 Hz, 1H), 7.98 (d, J= 2.4 Hz, 1H),7.45 (dd, J= 4.8 Hz, 1.2 Hz, 1H), 7.08 (d, J= 3.2 Hz, 1H), 6.98 (dd, J= 4.8 Hz, 3.2 Hz, 1H), 6.10 (t,J= 2.4 Hz, 1H). MS (M+H): 310 / 312.
The chemical industry reduces the impact on the environment during synthesis 58483-98-0, I believe this compound will play a more active role in future production and life.
Reference:
Patent; MERCK SHARP & DOHME CORP.; DAI, Xing; LIU, Hong; PALANI, Anandan; HE, Shuwen; NARGUND, Ravi; XIAO, Dong; ZORN, Nicolas; DANG, Qun; MCCOMAS, Casey C.; PENG, Xuanjia; LI, Peng; SOLL, Richard; WO2014/205593; (2014); A1;,
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