反应详情

To a solution of 7-iodo-2-(4-isopropylsulfonylphenyl)-5H-pyrrolo[2,3-b]pyrazine (5.0 g, 11.70 mmol) and DIPEA (3.024 g, 4.075 mL, 23.40 mmol) in DMF (25.00 mL) was added p-toluenesulfonyl chloride (2.454 g, 12.87 mmol). The resulting solution was stirred at room temperature for 2 hours. Water was added and the resultant precipitate collected, dried in vacuo at 40° C. to give the sub-title compound as an off-white solid (6.61 g, 97.16%). 1H NMR (400.0 MHz, DMSO) δ 9.18 (s, 1H), 8.64 (s, 1H), 8.42 (d, 2H), 8.05 (q, 4H), 7.48 (d, 2H), 3.50-3.45 (m, 1H), 2.36 (s, 3H) and 1.22-1.19 (m, 6H) ppm; MS (ES+) 581.9.

1. customthe resultant precipitate collected
2. customdried in vacuo at 40° C.