p-(Methylsulphonyl)benzoic acid → Diisopropylcarbodiimide

Participants

Reaction Steps

By carrying out the operation according to the procedure of Example 31, starting with 58.5 mg of 4-methylsulfonylbenzoic acid, 26.4 mg of hydroxybenzotriazole in solution in 0.5 cm3 of dimethylformamide, 0.0302 cm3 of diisopropyl-carbodiimide, a solution of 30 mg of 1-[bis(4-chlorophenyl)methyl]azetidin-3-ylamine in 0.5 cm3 of anhydrous dichloromethane, and 3 cm3 of anhydrous dichloromethane, N-{1-[bis(4-chlorophenyl)-methyl]azetidin-3-yl}-4-methylsulfonylbenzamide is obtained in the form of a white crystals [1H NMR spectrum (300 MHz, CDCl3, δ in ppm): 3.03 (mt: 2H); 3.09 (s: 3H); 3.61 (broad t, J=7.5 Hz: 2H); 4.35 (s: 1H); 4.73 (mt: 1H); 6.55 (broad d, J=7.5 Hz: 1H); from 7.20 to 7.35 (mt: 8H); 7.96 (d, J=8 Hz: 2H); 8.03 (d, J=8 Hz: 2H)].

Provenance & Evidence