4928-87-4, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, This compound has unique chemical properties. The synthetic route is as follows.
Example 2 1-(1-(1H-1,2,4-triazole-3-carbonyl)piperidin-3-yl)-3-methyl-8-(6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one 20 mg (0.0455 mmol) of Compound 111, 6.2 mg (0.0546 mmol) of 1H-1,2,4-triazole-3-carboxylic acid, 9.23 mg (0.0683 mmol) of HOBt and 13.09 mg of EDCI were suspended in 2 ml of dichloromethane, added with 13.9 mg (0.137 mmol) of triethylamine, and stirred at room temperature for 4 h. TLC (DCM: MeOH = 10: 1) showed that most of the raw materials were not reacted. 9.3 mg of 1H-1,2,4-triazole-3-carboxylic acid, 26 mg of HATU and 15 mg of triethylamine were supplemented, and stirred at room temperature overnight. TLC (DCM: MeOH = 10: 1) showed that most of the raw materials were reacted completely. 10 mL of saturated sodium bicarbonate solution was added and stirred for 1 h. The organic phase was separated off, and the aqueous phase was extracted with 2 * 5 ml of dichloromethane. The organic phases were combined, dried, evaporated to dryness, and purified by preparative TLC (dichloromethane: methanol = 10: 1) to afford the target compound of Example 2 (17.8 mg), as a light yellow powder. Yield: 73%. LC-MS: 535 [M+1]+, tR = 1.463 min. 1H NMR (400 MHz, DMSO+D2O) delta 9.41 (d, J = 7.9 Hz, 1H), 9.14 (d, J = 6.0 Hz, 1H), 9.00 – 8.91 (m, 1H), 8.87 – 8.79 (m, 1H), 8.78 – 8.65 (m, 2H), 8.64 – 8.44 (m, 2H), 8.39 (s, 1H), 8.22 – 7.96 (m, 1H), 5.56 – 4.07 (m, 3H), 4.00 (d, J = 16.3 Hz, 3H), 3.60 (d, J = 13.2 Hz, 3H), 3.44 – 3.17 (m, 2H), 3.00 – 2.82 (m, 1H), 2.31 – 2.14 (m, 1H).
If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.
Reference:
Patent; Beijing Forelandpharma Co. Ltd.; ZHANG, Xingmin; JI, Qi; WANG, Lei; GAO, Congmin; WANG, Ensi; DU, Zhenjian; GONG, Longlong; CHEN, Bo; (137 pag.)EP3072893; (2016); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics