反应详情

Carbonic acid 4-nitro-phenyl ester (S)-2,2,2-trifluoro-1-methyl-ethyl ester (85 mg) is added to a solution of (R)-5-(4-methanesulfonyl-phenyl)-2-piperidin-4-yl-2,3-dihydro-furo[2,3-c]pyridine (100 mg) and N,N-diisopropyl-ethylamine (60 μL) in tetrahydrofuran (2 mL) at room temperature. The solution is stirred at room temperature overnight and then washed with 1 N aqueous NaOH solution (3×), water, and brine. The organic phase is dried (MgSO4) and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 1:1→1:3) to give the title compound. LC (method 1): tR=1.00 min; Mass spectrum (ESI+): m/z=499 [M+H]+.

1. washwashed with 1 N aqueous NaOH solution (3×), water, and brine
2. dry with materialThe organic phase is dried (MgSO4)
3. concentrationconcentrated
4. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 1:1→1:3)