Reference of 1256785-86-0, 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.1256785-86-0, name is 1-(4-Aminopyridin-2-yl)ethanone, molecular formula is C7H8N2O, molecular weight is 136.15, as common compound, the synthetic route is as follows.
Example 20 (2R,5S)-N-(2-Acetyl-4-pyridyl)-4-(4-cyano-3-trifluoromethylphenyl)-2,5-dimethylpiperazine-1-carboxamide While stirring with ice-cooling, 12.5 ml of trifluoroacetic acid was added to 12.5 ml of chloroform solution containing 1.41 g of 2-acetyl-4-pyridinylcarbamic acid t-butyl ester.. The mixture was immediately warmed up to room temperature and stirred for 2 hours and 40 minutes.. The solvent was evaporated under reduced pressure to obtain a crude amine.. This compound was dissolved in 25 ml of pyridine, and the solution was mixed with 0.83 ml of phenyl chloroformate while stirring with ice-cooling and then immediately warmed up to room temperature.. After 8 hours and 30 minutes, this was mixed with 10 ml of pyridine solution containing 1.4 g of (2S,5R)-4-(2,5-dimethylpiperazin-1-yl)-2-trifluoromethylbenzonitrile and heated under reflux for 1 hour.. The reaction mixture cooled to room temperature was mixed with water and extracted with chloroform.. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate, and then the solvent was evaporated under reduced pressure.. The residue was purified by a silica gel column chromatography to obtain 1.03 g of the title compound from methanol-chloroform (1:99, v/v) elude. NMR: 1.10 (3H, d, J=7), 1.20 (3H, d, J=7), 2.61 (3H, s), 3.34-3.52 (2H, m), 3.75 (1H, d, J=14), 3.92 (1H, d, J=14), 4.28-4.45 (1H, m), 4.46-4.62 (I H, m), 7.20-7.35 (2H, m), 7.78-7.91 (2H, m), 8.12 (1H, d, J=2), 8.48 (1H, d, J=6), 9.24(1H, s)
The chemical industry reduces the impact on the environment during synthesis 1256785-86-0, I believe this compound will play a more active role in future production and life.
Reference:
Patent; Yamanouchi Pharmaceutical Co. Ltd.; US6673799; (2004); B1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem