反应详情

To a solution of 50 mg of 1-(1-ethyl-propyl)-2-thiophen-2-ylmethyl-1H-benzoimidazole-5-carboxylic acid in 2 ml of dry DMF 10 mg of HOAT, 35 mg of EDC and 0.1 ml of DIPEA were added at 0° C. After 15 min 25 mg of 1-pyridin-2-ylbutylamine were added and the reaction was stirred at rt for 16 h. The reaction was then poured into water and the pH was adjusted to 4 by the addition of 2 M aqueous hydrochloric acid. The reaction was extracted with ethyl acetate three times. The combined organic phases were dried over magnesium sulphate and concentrated. 70 mg (100%) of 1-(1-ethyl-propyl)-2-thiophen-2-ylmethyl-1H-benzoimidazole-5-carboxylic acid (1-pyridin-2-yl-butyl)-amide were obtained.

1. extractionThe reaction was extracted with ethyl acetate three times
2. dry with materialThe combined organic phases were dried over magnesium sulphate
3. concentrationconcentrated