1-Hydroxybenzotriazole → [(2R)-1-({2-[(2-furylmethyl)amino]-6-methylpyridin-3-yl}carbonyl)pyrrolidin-2-yl](diphenyl)methanol

Participants

Reaction Steps

To a solution of 2-[(2-furylmethyl)amino]-6-methylnicotinic acid (13.9 mg) and diphenyl(pyrrolidin-2-yl)methanol (18.2 mg) in DMF (1.0 ml) was added a solution of HOBt (9.7 mg) and WSC.HCl (13.8 mg) in DMF (0.5 ml), and the mixture was stirred at room temperature overnight. The reaction mixture was poured into 2% aqueous sodium hydrogen carbonate, the mixture was extracted with ethyl acetate, and the extract was concentrated by a nitrogen gas blower. The residue was subjected to reversed-phase preparative HPLC, and the object fraction was passed through MP-CO3 resin (manufactured by Polymer Laboratories) to remove trifluoroacetic acid. The obtained solution was concentrated by a nitrogen gas blower to give the object compound (10.6 mg).

Provenance & Evidence