Application of 16681-67-7, 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. 16681-67-7, name is 4-Bromo-2-methyl-2H-1,2,3-triazole, molecular formula is C3H4BrN3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.
4H-[l,2,4]triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-(4R)-l,4-dimethyl-8-(2- methyl- 2H-l,2,3-triazole-4-yl)-6-(4-chloro-phenyl) (Compound 48). A mixture of 4-R-4H- [l,2,4]triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-l,4-dimethyl-8-(4,4,5,5- tetramethyl-1.3.2- dioxaborolan-2-yl)-6-(4-chloro-phenyl) (200 mg, 0.44 mmol), 4-bromo-2-methyl-2H-1.2.3- triazole (72 mg, 0.44 mmol), tetrakis(triphenylphosphine)palladium(0) (51 mg) and potassium carbonate (243 mg, 1.76 mmol) in mixed solution of tetrahydrofuran (10 mL) and water (2 mL) was heated at 100C for 30 minutes under microwave (pressure: 17.2 bar, equipment power : 150W). The reaction mixture was diluted with ethyl acetate (50 mL), washed by brine (20 mL x 3), dried over anhydrous sodium sulfate and then filtered. The filtrate was concentrated and the residue was purified by column chromatography (silica gel,dichloromethane/methanol = 10:1) to afford 4-R-4H-[ 1,2,4] triazolo[4,3-a][l,5]benzodiazepine, 5,6-dihydro-l,4-dimethyl-8-(2-methyl-2H-l,2,3-triazole-4-yl)-6-(4-chloro-phenyl) as a white solid (80 mg, 44.5 %).
Therefore, this conceptually novel strategy might open impressive avenues to establish green and sustainable chemistry platforms.In my other articles, you can also check out more blogs about 4-Bromo-2-methyl-2H-1,2,3-triazole.
Reference:
Patent; CONSTELLATION PHARMACEUTICALS, INC.; ALBRECHT, Brian, K.; GEHLING, Victor, S.; HEWITT, Michael, C.; TAYLOR, Alexander, M.; HARMANGE, Jean-Christophe; WO2012/151512; (2012); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics