Related Products of 288-36-8, These common heterocyclic compound, 288-36-8, name is 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.
A mixture of methyl 5-chloro-6-methoxy-3-[(4-methyl-l-naphthoyl)amino]pyrazine-2- carboxylate prepared in Example 25E (0.258 g, 0.67 mmol, 1 eq.), JV-bromosuccinimide (0.123 g, 0.69 mmol, 1.0 eq.) and benzoyl peroxide (0.018 g, 0.07 mmol, 0.11 eq.) in 100 mL carbon tetrachloride was refluxed for 1 h until LC/MS showed that bromination was complete. The reaction mixture was cooled to 50 0C and 1,2,3-triazole (0.245 g, 3.55 mmol, 5.3 eq.) was added. The resulting mixture was stirred at 80 0C for 2 h until LC/MS showed that the reaction was complete. The solvents were removed in vacuo. The residue was dissolved in 10 mL dimethyl sulfoxide. The resulting dimethyl sulfoxide solution was purified by reversed-phase preparative HPLC. Freeze drying gave 0.062 g (21 %) of title compound.1H NMR (400 MHz, DMSO-*) delta (ppm) 3.80 (s, 3H), 4.01 (s, 3H), 5.72 (s, IH), 6.16 (s, 2H), 7.37 (d, J=7.2 Hz, IH), 7.63 (m, 2H), 7.71 (d, J=7.3 Hz, IH), 7.73 (s, IH), 8.18 (s, IH), 8.26 (m, 2H), 11.41 (br s, IH).
The synthetic route of 288-36-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; WO2007/61360; (2007); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics