Electric Literature of 16681-70-2, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 16681-70-2, name is 1H-[1,2,3]Triazole-4-carboxylic acid, molecular formula is C3H3N3O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
HATU (79 mg, 207 .imol) was added to a stirred solution of 1H-1,2,3-triazole-4- carboxylic acid (23 mg, 207 .imol) in DMF (1.3 mL) and stirred for 10 minutes. DIPEA (49 mg, 376 .imol) was added and after 5 minutes, Compound 2 (66 mg, 188 .imol) pre5 dissolved in DMF and DIPEA (1.3 mL, 2 eq.) was added. After 90 minutes LCMSindicated the major product. The mixture was then concentrated in vacuo. The product was determined to be a mixture of the isomers with an additional impurity. The product was purified by preparative HPLC to yield the title isomer a (2.75 mm retention time; 1.1 mg) and b (2.68 mm retention time; 3.1 mg) as TFA salts.
The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about 1H-[1,2,3]Triazole-4-carboxylic acid, hurry up and to see.
Reference:
Patent; THERAVANCE BIOPHARMA R&D IP, LLC; FLEURY, Melissa; BEAUSOLIEL, Anne-Marie; HUGHES, Adam D.; LONG, Daniel D.; WILTON, Donna A.A.; WO2015/116760; (2015); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics