2-chloro-5-fluorobenzenesulfonyl chloride

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: The title compound was prepared according to the procedure described for Example 84 starting from tert-butyl trans-4-[(5-amino-1-benzofuran-7-yl)oxy]-3-fluoropiperidine-1-carboxylate (Intermediate 53) and 2-chloro-5-fluorobenzenesulfonyl chloride. Yield: 34 mg (18%), HPLC purity=100%, m/z=443 (M+H)+, 1H NMR (270 MHz, methanol-d4) δ ppm 2.11-2.36 (m, 2H) 3.15-3.58 (m, 3H) 3.63-3.81 (m, 1H) 4.77-4.98 (m, 1H) 5.00-5.24 (m, 1H) 6.75 (d, J=2.23 Hz, 1H) 6.85 (d, J=1.98 Hz, 1H) 7.05 (d, J=1.98 Hz, 1H) 7.09-7.20 (m, 1H) 7.42 (dd, J=8.66, 2.47 Hz, 1H) 7.72 (d, J=2.23 Hz, 1H) 7.97-8.06 (m, 1H).