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N-[4-(pyridine-4-yloxy)phenyl]-5-methyl-1H-benzimidazole-2-carboxamide[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
39.5%
0.064 mmol of BENZIMIDAZOLECARBOXYLIC ACID 4K WAS DISSOLVED in DMF together with 0.064 mmol of the amine 5a, a solution of TBTU (0.096 MMOL) in DMF, HOBT (0.026 MMOL) in DMF and 0.32 mmol of DIPEA were added successively, and the mixture was stirred at room temperature. After 4 hours, 0.3 eq. of acid was added, and the mixture was stirred overnight. After further addition of 0.3 eq. of acid, the reaction mixture was diluted with water after 2 hours, and the resulting precipitate was filtered off with suction and washed with water. The resulting crude product was purified by chromatography (ethyl acetate/n-heptane: 9/1). Yield : 39.5%, beige solid