312-73-2, name is 2-(Trifluoromethyl)-1H-benzo[d]imidazole, belongs to imidazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Safety of 2-(Trifluoromethyl)-1H-benzo[d]imidazole
The 4-(4-aminopiperidin- 1 -yl)-6-morpholino-2-(2-trifluoromethylbenzimidazol- l-yl)pyrimidine dihydrochloride used as a starting material was prepared as follows :- Under an atmosphere of nitrogen, a mixture of 2-trifluoromethyl- 1 H-benzimidazole(2 g), 2,4-dichloro-6-morpholinopyrimidine (2.79 g), sodium bicarbonate (4 g) and DMA (28 ml) was heated to 110C in a sealed vessel in a microwave oven for 18 hours. The reaction mixture was heated to 140C for 20 hours and to 160C for 48 hours. The solvent was evaporated from the resultant reaction mixture. The residue was partitioned between ethyl acetate and water. The organic solution was washed in turn with water and with a saturated aqueous sodium chloride solution. The organic solution was dried over anhydrous sodium sulphate and evaporated. The resultant product was purified using a Waters ‘Xterra’ preparative reversed-phase column (5 microns silica, 19 mm diameter, 100 mm length) and decreasingly polar mixtures of a 1% solution of ammonium hydroxide (d=0.88) in water and acetonitrile as eluent. There was thus obtained 4-chloro-6-morpholino-2-(2-trifluoromethylbenzimidazol-l-yl)pyrimidine (0.65 e): NMR Spectrum: (DMSOd6) 3.75
The synthetic route of 312-73-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; BUTTERWORTH, Sam; GRIFFEN, Edward, Jolyon; PASS, Martin; WO2008/32028; (2008); A1;,
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