3-(2-Methoxy-5-methylphenyl)-3-phenylpropyl 4-methylbenzenesulfonate

Conditions: temp:80.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: The compound, toluene-4-sulphonic acid-3-(2-methoxy-5-methylphenyl)-3-phenylpropyl ester (prepared as described in EP 0325571, 1.5 gm, 3.66 mmole, 1 eq) was dissolved in dry acetonitrile (4 ml). To the reaction mixture, 3-benzyl-3,6-diazabicyclo[3.1.0]hex-6-yl amine, 1.38 gm, 7.32 mmole, 2 eq, (prepared according to T. F. Braish et al. Synlett 1996, 1100) and triethylamine (5.1 ml) were added. The resulting reaction mixture was heated at 80° C. for 4 days. The solvents were evaporated off, from the reaction mixture under reduced pressure. The residue was dissolved in ethyl acetate, and washed with saturated sodium bicarbonate solution. The organic layer was separated, dried over sodium sulphate and concentrated under high vaccum. The crude compound was purified through column chromatography using ethyl acetate in hexane solvent system. were added The resulting reaction mixture The solvents were evaporated off, from the reaction mixture under reduced pressure The residue was dissolved in ethyl acetate washed with saturated sodium bicarbonate solution The organic layer was separated dried over sodium sulphate concentrated under high vaccum The crude compound was purified through column chromatography