反应详情

Using similar reaction conditions as described in, step ii of Intermediate 1, tert-butyl 4-(2-fluoro-4-(3-iodo-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperidine-1-carboxylate (400 mg, 0.767 mmol) was tosylated with p-toluene sulfonylchloride (220 mg, 1.151 mmol) and DMAP (282 mg, 2.303 mmol) in DCM (20 mL) to afford 250 mg (48.26% yield) of the titled compound after purification with (60/120 silica gel) column chromatography using 1% methanol in DCM as eluent. MS: m/z=676.3 (M+1). 1H NMR (CDCl3, 300 MHz): δ 8.619-8.611 (d, 1H), 8.12-8.09 (d, 2H), 7.89 (s, 1H), 7.767-7.760 (d, 1H), 7.31-7.23 (m, 5H), 4.26 (s, 2H), 3.08-3.00 (m, 1H), 2.95-2.75 (m, 2H), 2.38 (s, 3H), 1.86-1.64 (m, 4H), 1.489 (s, 9H).

1. customreaction conditions