4-prop-2-ynyl-1,4-thiazinane 1-oxide

反応条件: temp:50.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Prepared from N-propargyl S-oxo-4-thiapiperidine (30.5 mg, 0.194 mmol) and 3-fluoro-4-(2-iodothieno[3,2-b]pyridin-7-yloxy)benzenamine (Example 6, Step A; 50 mg, 0.13 mmol) according to the procedure described for Example 6, Step B, except the reaction was heated at 50° C. for 7 hours. The crude was purified by preparative TLC [5% MeOH (containing 7N NH3) in CH2Cl2]. The product was obtained as a waxy solid (45 mg, 74%). 1H NMR (400 MHz, CDCl3) δ 8.48 (d, J=6 Hz, 1H), 7.61 (s, 1H), 7.03 (m, 1H), 6.53 (m, 2H), 6.47 (m, 1H), 3.89 (br s, 2H), 3.64 (s, 2H), 3.25 (m, 2H), 2.92 (m, 6H). The crude was purified by preparative TLC [5% MeOH (containing 7N NH3) in CH2Cl2]