Synthetic Route of 10325-70-9, 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.10325-70-9, name is 5-Acetylpyrimidine, molecular formula is C6H6N2O, molecular weight is 122.1246, as common compound, the synthetic route is as follows.
Preparation 84 (R)-N-((5)-2-(2,4-difluorophenyl)-4-oxo-4-(pyrimidin-5-yl)butan-2-yl)-2-methylpropane- 2-sulfinamide To a solution of l-(pyrimidin-5-yl)ethanone (2.072 g, 16.97 mmol) in DMF (40 mL) was added 60 % wt aH (0.747 g, 18.66 mmol) at 0 C under nitrogen. The mixture was stirred at 0 C for 30 min. A solution of (R,¡ê)-N-(l-(2,4-difluorophenyl)ethylidene)-2- methylpropane-2-sulfinamide from preparation 73 (2.2 g, 8.48 mmol) in DMF (4 mL) was slowly added at -10 C under nitrogen. The mixture was stirred from -10 C to -5 C over 1.5 h. The reaction was quenched with water, and extracted with 2×250 mL of ethyl acetate. The combined organic layers were removed, dried over sodium sulfate, and concentrated. The residue was purified via silica gel chromatography (gradient elution using ethyl acetate to 10% methanol in ethyl acetate) to give (R)-N-((5)-2-(2,4- difluorophenyl)-4-oxo-4-(pyrimidin-5-yl)butan-2-yl)-2-methylpropane-2-sulfinamide (1.5 g, 3.93 mmol, 46.4 % yield). MS (M+H)+ = 382.05. 1H NMR (500MHz, CHLOROFORM-d) delta 9.37 (s, 1H), 9.18 (s, 2H), 7.61 (td, J=9.3, 6.5 Hz, 1H), 6.97 – 6.89 (m, 1H), 6.74 (ddd, J=12.9, 8.4, 2.6 Hz, 1H), 5.32 (s, 1H), 4.21 (dd, J=18.6, 1.4 Hz, 1H), 3.91 (dd, J=18.6, 2.9 Hz, 1H), 1.86 (s, 3H), 1.34 (s, 9H).
The chemical industry reduces the impact on the environment during synthesis 10325-70-9, I believe this compound will play a more active role in future production and life.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; WU, Yong-Jin; GUERNON, Jason M.; WO2014/98831; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia