Hydrochloric Acid → HCID 68671111, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 6-({(2E)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-3-[(2R,3R,7S)-2,3-diphenyl-1,4-dioxaspiro[4.4]non-7-yl]prop-2-enoyl}amino)nicotinic acid (194 mg) in 1,4-dioxane (4 mL) was added 4 M hydrochloric acid (4 mL), followed by stirring at 50° C. for 2 hours. After leaving it to be cooled to room temperature, saturated brine was added thereto. After extraction with chloroform, the organic layer was dried over anhydrous magnesium sulfate. The crude product obtained by concentration was dissolved in ethyl acetate (4 mL), and 4 M hydrogen chloride/ethyl acetate (1 mL) was added thereto. It was stirred at room temperature for 30 minutes and concentrated. The obtained oily substance was solidified with diisopropyl ether and collected by filtration to obtain 6-({(2E)-2-[3-cyclopropyl-4-(cyclopropylsulfonyl)phenyl]-3-[(1S)-3-oxocyclopentyl]prop-2-enoyl}amino)nicotinic acid monohydrochloride (87 mg) as a white solid.

Provenance & Evidence