New downstream synthetic route of 27808-16-8

The synthetic route of 27808-16-8 has been constantly updated, and we look forward to future research findings.

Related Products of 27808-16-8, These common heterocyclic compound, 27808-16-8, name is 4-Methyl-1H-1,2,3-triazole, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

4-Methyl-1 H-1 ,2,3-triazole (0.1 1 mL, 1 .85mmol) was added to a solution of 3-bromo-6- methylpyridine-2-carboxylic acid (200. mg, 0.930mmol) in 1 ,4-Dioxane (1 mL)/ Water (0.1 ml_), followed by Cul (8.86mg, 0.050mmol), (1 R,2R)-N 1 , N2-dimethylcyclohexane-1 ,2- diamine (26.34mg, 0.190mmol) and cesium carbonate (607.03mg, 1 .85mmol The mixture was stirred at 120 C for 5 h. Reaction mixture was cooled to room temperature and then water and MTBE were added. After vigorously stirring, the layers were separated and the aqueous one was acidified to pH 2 with HCI 6N. The acidic solution was concentrated and purified by RP on C18 column [H20 (0.1 % HCOOH)/Acetonitrile=60/40] affording 6-methyl-3-(4-methyltriazol-2-yl)pyridine-2- carboxylic acid (p64, 139 mg, y= 69% yield) as a white solid. MS (mlz): 219.2 [MH]+.

The synthetic route of 27808-16-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; CHRONOS THERAPEUTICS LIMITED; MICHELI, Fabrizio; CREMONESI, Susanna; SEMERARO, Teresa; TARSI, Luca; GIBSON, Karl Richard; (116 pag.)WO2019/81939; (2019); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics