Acetic Acid → 1-Biphenyl-2-yl-4-(2-trifluoromethyl-benzenesulfonyl)-pyrrolidine-2-carboxylic Acid Ethyl Ester

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Reaction Steps

Paraformaldehyde (74 mg, 2.4 mmol) was added to a solution of (biphenyl-2-ylamino)-acetic acid ethyl ester (125 mg, 490 umol; CAS Reg. No. 39950-19-1) in toluene (9 ml) under an argon atmosphere. The mixture was stirred for 1 h at ambient temperature. A solution of 1-ethenesulfonyl-2-trifluoromethyl-benzene (231 mg, 979 umol) in toluene (1 ml) and acetic acid (10 ul, 98 umol) were added and the reaction mixture was heated under reflux conditions to 120° C. for 12 h. The solvent was removed under reduced pressure and purified by column chromatography (silica gel, EtOAc/heptane) to obtain the title compound (47 mg, 93 umol; 19%) as colorless oil. MS (ESI): m/z=504.1 [M+H]+.

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