Reagents and conditions: (a) LHMDS, THF, -78 °C to rt, 20%; (b) 2-aminonicotinaldehyde or 2-aminobenzaldehyde, KOH, EtOH, reflux, 47%. (c) ethylsulfonylethene, TEA, MeOH, reflux; (d) 4-fluoro-3-trifluoromethylphenylacetic acid, EDC, HOBt, NMM, DMF, rt, 80–90% two steps. (e) Pd(PPh3)4, CuI, NaCN, MeCN, microwave, 120 °C, 80–90%. Enantiomerically pure products were isolated by chiral phase HPLC.