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1H-Benzimidazol-2-amine,1-butyl-(9CI) synthesis

3synthesis methods
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Yield:91337-45-0 74%

Reaction Conditions:

with potassium hydroxide in acetone at 60; for 3 h;

Steps:

Synthesis of l-butyl-lH-benz[i ]imidazol-2-amine (Compound A8a).

To a solution of 2- aminobenzimidazole (compound A7) (27 mg, 0.2 mmol) in acetone (1 mL) were added KOH (22 mg, 0.4 mmol) and butyl iodide (23 //L, 0.2 mmol). The reaction mixture was stirred for 3 h at 60 °C. The reaction mixture was cooled to room temperature and the solvent was removed under reduced pressure. The reaction mixture was diluted with water and extracted with EtOAc (3 x 10 mL). The combined organic layer was dried over Na2S04, concentrated under reduced pressure, and the crude material was purified by silica gel column chromatography (20%> MeOH/CH2Cl2) to obtain the compound A8a as a white solid (28 mg, 74%). Rf = 0.45 (20% MeOH/CH2Cl2).

References:

WO2015/23958,2015,A1 Location in patent:Page/Page column 57