Application of 1124-29-4, 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.1124-29-4, name is 5-Acetylpyridin-2(1H)-one, molecular formula is C7H7NO2, molecular weight is 137.14, as common compound, the synthetic route is as follows.
[0561] To a solution of III-3 (1 eq.) in DCM (0.1 mmol/mL) was added boronic acid III-4 (2 eq.), Cu(OAc)2 (1 eq), Pyridine (10 eq.) and Pyridine-N-Oxide (2 eq.), followed by addition of 4 molecular sieve (quantity approx. equal to III-3). The reaction mixture was stirred at rt under oxygen atmosphere overnight. After completion of the reaction indicated by TLC, the resulting mixture was filtered and washed with, the filtrate was washed with brine, dried over Na2SO4 and concentrated. The residue was purified by column chromatography on silica gel to give III-5 [0572] Compound 20 was prepared following the general procedure, except the solvent was changed to acetonitrile (10% yield). 1H NMR (CDCl3, 400 MHz) delta 8.06 (d, J=2.4 Hz, 1H), 7.97 (dd, J=10, 2.4 Hz, 1H), 7.53-7.45 (m, 1H), 7.43-7.36 (m, 1H), 7.34-7.25 (m, 2H), 6.67 (d, J=10 Hz, 1H), 2.45 (s, 3H). MS (ESI) m/z (M+H)+ 232.0.
The chemical industry reduces the impact on the environment during synthesis 1124-29-4, I believe this compound will play a more active role in future production and life.
Reference:
Patent; Buckman, Brad Owen; Nicholas, John Beamond; Ramphal, Johnnie Y.; Emayan, Kumaraswamy; Seiwert, Scott D.; US2014/94456; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem