4928-87-4, name is 1,2,4-Triazole-3-carboxylic acid, belongs to triazoles compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. category: Triazoles
A mixture of 50 mg (0.045 mmol) of compound 136 hydrochloride, 18.8 mg (0.166 mmol) of 1 H-1,2,4-triazol-22.4 mg (0.166 mmol)H0Bt and 31.8 mg EDCISuspended in 4mlTwo gas a burning,Add 58.8 mg(0.581 mmol) of triethylamine,Stirred at room temperature overnight,TLC (DCM: Me0H = 10: l)Showing that most of the raw materials did not react,Additional10 mg of 1H-1,2,4-triazole-3-carboxylic acid,47 mg of HATU and 30 mg of triethylamine,Stirred at room temperature overnight,TLC (DCM: Mu0Eta =10: 1) shows most of the raw material reaction finished,Add 15ml saturated sodium bicarbonate solution for 0.5 hours, the organic phase, the water phase(5: 10) dichloromethane methanol mixture (about 10: 1) extraction, and then 2 1 10 ml of dichloromethane extraction, combined organic phase, dryDry, filtered, evaporated to dryness, preparative TLC purification (dichloromethane: methanol = 10: 1)To give the title compound of Example 51,11mg light yellowThe yield was 21.2%.
The synthetic route of 4928-87-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Beijing Foreland Pharma Co., Ltd; Zhang, Xingmin; Wang, Ensi; Niu, Shengxiu; Guo, Jing; Dai, Zhuolin; Zheng, Nan; Ji, Qi; Li, Qinyan; Liang, Tie; (109 pag.)CN104411706; (2016); B;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics