A new synthetic route of 799842-07-2

At the same time, in my other blogs, there are other synthetic methods of this type of compound,799842-07-2, N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, and friends who are interested can also refer to it.

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.799842-07-2, name is N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, molecular formula is C16H19BrFN3O2S, molecular weight is 416.31, as common compound, the synthetic route is as follows.Product Details of 799842-07-2

b) from PMDBR (Kornblum oxidation): NaHC03 (220 mg, 2.6 mmol, 1.1 equiv.) and Nal (10 mol %) were dissolved in DMSO (5 mL) and cooled to 20 C. Then, PMDBR (1.0 g, 2,4 mmol, 1 equiv.) in DMSO (5 mL) was slowly added via a syringe pump during 1 h and reaction was left to stir for 24 h. Reaction mixture was then warmed to 70 C and Ac20 (5 equiv.) was added dropwise. Reaction was left to stir for additional 3 hours. After cooling on an ice bath, water (20 mL) was slowly added and precipitate was filtered off to afford 0.78 g (93 %) of PMDCHO.1H NMR (CDCI3): delta 1.30 (6H, d, J = 6.7 Hz), 3.53 (3H, s), 3.62 (3H, s), 3.99 (1 H, sep, J = 6.7 Hz), 7.21 (2H, m), 7.61 (2H, m), 9.95 (1 H, s) ppm. 13C NMR (CDCI3): 521.6, 31.9, 33.0, 42.4, 115.8, 116.0, 119.5, 132.5, 132.6, 158.7, 163.1 , 165.6, 169.7, 178.9, 190.4 ppm.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,799842-07-2, N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, and friends who are interested can also refer to it.

Reference:
Patent; LEK PHARMACEUTICALS D.D.; CASAR, Zdenko; STERK, Damjan; JUKIC, Marko; WO2012/13325; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia