1-Hydroxybenzotriazole → (E)-3-[5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl]-N-(2-oxo-3-phenyl-tetrahydropyrimidin-1-yl)acrylamide

Participants

Reaction Steps

1-Amino-3-phenyl-tetrahydropyrimidin-2-one synthesized by the same method as in Example 232 at room temperature (111 mg; ESI-MS; m/z 192 [M++H]), IPEA (0.41 mL), EDC (166 mg) and HOBT (117 mg) were added to a solution of (E)-3-[5-methoxy-6-(4-methyl-1H-imidazol-1-yl)pyridin-3-yl]acrylic acid (300 mg) in DMF (6 mL). The reaction solution was stirred at room temperature for 24 hours. The reaction solution was diluted with ethyl acetate and washed with a saturated sodium bicarbonate solution and a saturated sodium chloride solution. The resulting organic layer was dried over magnesium sulfate and then concentrated under reduced pressure. The residue was purified by silica gel column chromatography (carrier: Chromatorex NH; elution solvent: heptane-ethyl acetate system, then ethyl acetate-methanol system) to obtain 250 mg of the title compound. The property value of the compound is as follows.

Provenance & Evidence