These common heterocyclic compound, 5805-57-2, name is (1H-Benzo[d]imidazol-2-yl)methanamine, 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. Quality Control of (1H-Benzo[d]imidazol-2-yl)methanamine
The solution of Boc-( )-3-amino-4-(2,4-dichlorphenyl)butyric acid (30 mg , 0,086 mmoL 1 ,0 equiv), DIPEA ( 3 equiv), EDC HCi ( 1.5 equiv) and DMAP (1.0 equiv) in DCM (20 mL) was stirred for 1 Grain. To this reaction mixture ( 1 H-benzo[d]imidazol-2- yljmethanamine (1 .0 equiv) was added. The reaction mixture was stirred at room temperature overnight. The organic layer was washed with aq NaHC03 and brine. It was then dried over anhydrous sodium sulfate and evaporated under vacuum. The residue was purified by flash column chromatography. The above purified compound was dissolved in 3 ml of DCM, To the solution, 1 ml of TFA was added dropwise. The solution was stirred for 40 min at room temperature. The reaction mixture was evaporated under vacuum, neutralized with aq aHC03 and extracted with ethyl acetate. The ethyl acetate layer was dried over anhydrous sodium sulfate and concen (M – i i , 378.3.
The synthetic route of (1H-Benzo[d]imidazol-2-yl)methanamine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; UNIVERSITY OF WASHINGTON; BUCKNER, Frederick, S.; ALVAREZ, Ximena, Barros; FAN, Erkang; GILLESPIE, John, Robert; HOL, Wilhelmus, G.J.; HUANG, Wenlin; KOH, Cho, Yeow; RANADE, Ranae, M.; SHIBATA, Sayaka; VERLINDE, Christophe, L.M.; ZHANG, Zhongsheng; (249 pag.)WO2016/29146; (2016); A1;,
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