反应详情

A solution of the mixture of diastereomers of tert-butyl 3-(3,4-dichlorophenyl)-4-(1-((R)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazine-4-carbonyl)pyrrolidine-1-carboxylate (34 mg, 0.061 mmol) in DCM (3.1 mL) was added to a 4.0M HCl solution in dioxane (1.1 mL, 4.25 mmol). The mixture was stirred at room temperature overnight. The solvents were removed in vacuo to give ((3S,4R)-4-(3,4-dichlorophenyl)pyrrolidin-3-yl)(4-((R)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)methanone dihydrochloride and ((3R,4S)-4-(3,4-dichlorophenyl)pyrrolidin-3-yl)(4-((R)-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)methanone dihydrochloride as a mixture of diastereomers (32 mg, 99%).

1. customThe solvents were removed in vacuo