Hydrochloric Acid → HCID 178477325, compound

Participants

Reaction Steps

A solution mixture of 7.2 g 2-(ethylsulfanyl)-6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]-1H-benzo[d]imidazole obtained in Production Example 73, 3.5 g 4-fluorophenylboronic acid, 3.4 g copper (II) acetate, 2.0 mL pyridine, 4.6 g of 4 Å molecular sieves and 140 mL dichloromethane was stirred at room temperature for 96 hours. The reaction mixture was filtered through Celite, the solvent was evaporated, and the residue was purified by silica gel chromatography (hexane/ethyl acetate) to give 1.06 g 2-(ethylsulfanyl)-1-(4-fluorophenyl)-6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]-1H-benzo[d]imidazole as colorless crystals. 30 mg of 2-(ethylsulfanyl)-1-(4-fluorophenyl)-6-[3-(4-fluorophenyl)-1-trityl-1H-4-pyrazolyl]-1H-benzo[d]imidazole was subjected to deprotection of the trityl group and converted into the corresponding hydrochloride by the same method as in Example 67, to give 13 mg of the title compound as colorless crystals.

Provenance & Evidence