A common heterocyclic compound, 13273-53-5, name is 4-Bromo-1-methyl-1H-1,2,3-triazole, molecular formula is C3H4BrN3, 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. 13273-53-5.
A mixture of methyl 2-(3-fluoro-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetate (288 mg), 4-bromo-1-methyl-1H-1,2,3-triazole (132 mg), PdCl2(dppf) (30.3 mg), 2M aqueous potassium carbonate solution (1.0 mL) and toluene (4.0 mL) was stirred under a nitrogen atmosphere at 100C for 2 hr. The insoluble material was filtered off, water was added to the filtrate at room temperature, and the aqueous layer was extracted with ethyl acetate. The organic layer was washed with water and saturated brine, and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (NH, ethyl acetate/hexane) to give the title compound (70.3 mg). MS: M+1 250.1.
The synthetic route of 4-Bromo-1-methyl-1H-1,2,3-triazole has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Takeda Pharmaceutical Company Limited; HIRAYAMA, Takaharu; HIRATA,Yasuhiro; TOMINARI, Yusuke; IWAMURA, Naoki; SASAKI, Yusuke; ASANO, Moriteru; TAKAGI, Terufumi; OKANIWA,Masanori; YOSHIDA, Masato; IMAMURA, Shinichi; (64 pag.)EP3514150; (2019); A1;,
1,2,3-Triazole – Wikipedia,
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