Imidazole → HCID 17808988, compound

Participants

Reaction Steps

To a solution of imidazole (330 mg) in dimethylformamide (0.74 ml) is added trimethylsilyl chloride (0.61 ml) at room temperature, and the mixture is stirred for 20 minutes. To the solution is added 4-amino-5-chloro-2-methoxy-N-[1-(4-piperidinylmethyl)-4-piperidinyl]-benzamide (610 mg), and the mixture is stirred at room temperature for 24 hours. To the reaction mixture is added a small amount of water, and the mixture is concentrated to dryness under reduced pressure. To the residue is added water, and the mixture is extracted with chloroform. The organic layer is washed with a saturated aqueous sodium chloride solution, dried over anhydrous sodium sulfate, and the solvent is evaporated under reduced pressure. The residue is purified by silica gel column chromatography (eluent; chloroform:methanol=30:1→20:1) to give the desired compound (200 mg) as amorphous.

Provenance & Evidence