These common heterocyclic compound, 57667-50-2, name is 1-Propyl-1H-benzo[d]imidazol-2-amine, 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. Formula: C10H13N3
1 -Propyl- lH-benzimidazol-2-amine (0.600 g, 3.42 mmol), 3-({[(l,l- dimethylethyl)oxy]carbonyl}amino)benzoic acid (0.894 g, 3.77 mmol), EDC (0.722 g, 3.77 mmol), and EtaOAT (0.513 g, 3.77 mmol) were suspended in DMF (10 mL), followed by addition of NMM (0.414 mL, 3.77 mmol). After stirring at room temperature for 72 h, the contents were concentrated in vacuo and the crude product purified by reverse phase EtaPLC (used non-TFA containing mobile phase). The product was collected as a white solid (0.791 g, 59%). LC-MS (ES) m/z = 395.0 (M+Eta)+ 1H NMR (400 MHz, DMSOd6) delta ppm 12.71 (s, IH), 9.46 (s, IH), 8.36 (s, IH), 7.83 (d, J = 7.6 Hz, IH), 7.62 (d, J = 7.6 Hz, IH), 7.51-7.54 (m, 2H), 7.33-7.35 (m, IH), 7.21- 7.25 (m, 2H), 4.23 (t, J = 6.9 Hz, 2H), 1.92-1.95 (m, 2H), 1.50 (s, 9H), 0.94 (t, J = 7.3 Hz, 3H).
The synthetic route of 1-Propyl-1H-benzo[d]imidazol-2-amine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXOSMITHKLINE LLC; LAFRANCE, Louis, Vincent; LEBER, Jack, Dale; LI, Mei; VERMA, Sharad, Kumar; WO2010/126922; (2010); A1;,
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