Related Products of 16681-67-7, These common heterocyclic compound, 16681-67-7, name is 4-Bromo-2-methyl-2H-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.
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 %).
Statistics shows that 4-Bromo-2-methyl-2H-1,2,3-triazole is playing an increasingly important role. we look forward to future research findings about 16681-67-7.
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