Imidazole → HCID 15347011, compound

Participants

Reaction Steps

500 mg (1.01 mmol) of Compound 59 obtained in Example 59 was dissolved in 10 ml of tetrahydrofuran, 137 mg imidazole and 80 mg of sodium hydride (60% oil dispersion) were added and the mixture was heated at reflux for 2.3 hours. At 1.5 hours after the reaction was started, 40 mg of sodium hydride (60% oil disperison) was added. An aqueous solution of ammonium chloride was added to the reaction solution and the mixture was extracted with chloroform. The organic layer was washed with an aqueous saturated solution of sodium chloride and dried over anhydrous sodium sulfate and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (chloroform:methanol:triethylamine=200:10:1) and triturated with n-hexane to give Compound 64 which was converted into hydrochloride according to the same manner as that in Example 16 to give 447 mg (73%).

Provenance & Evidence