2849-93-6, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 2849-93-6 as follows.
Diisopropylethylamine (2.2 [MMOL)] was added to a solution of benzimidazole-2- carboxylic acid (3.59 [MMOL),] [0- (7-AZABENZOTRIAZOL-1-YL)-N, N, N’, N’-] [TETRAMETHYLURONIUM] hexafluorophosphate (HATU, 3.00 [MMOL),] 1-hydroxy-7- [AZABENZOTRIAZOLE] (HOAT, 3.00 [MMOL),] and 1-methylpiperazine (2.00 [MMOL)] in DMF (0.5 M). The reaction mixture was allowed to stir at room temperature overnight. The solvent was removed, and the residue was dissolved in EtOAc. The solution was washed with 1 N HCI, satd aq [NAHCO3] and brine. It was then dried [(NA2SO4),] filtered, and concentrated to obtain the crude product as a viscous oil, which was purified on silica gel (40 g; 3-10% methanol (2 M NH3)/dichloromethane), yielding the title compound (1.68 mmol, 47%). Elemental analysis: calculated for [C13H16N4O,] C 63.91, H 6.60, N 22.93 ; found C 63.76, H 6.79, N 22.87. The MS [AND 1H] NMR data matched that of the sample prepared above.
According to the analysis of related databases, 1H-Benzimidazole-2-carboxylic acid, the application of this compound in the production field has become more and more popular.
Reference:
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2004/22060; (2004); A2;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem