反应详情

温度

160 °C

A mixture of 2-butyl-4-chloro-5-phenylisothiazol-3(2H)-one 1,1-dioxide (1.000 g, 3.336 mmol), tert-butyl 5-amino-1-benzofuran-2-carboxylate (0.778 g, 3.336 mmol) and TEA (0.340 ml, 2.471 mmol) in MeCN (5 ml) was heated in a microwave reactor at 160° C. for 1.5 h. The reaction mixture was evaporated and the residue was purified by flash chromatography using 5:1 DCM/EtOAc (+1% AcOH) as eluent to give the title compound (0.425 g, 29%). 1H NMR (500 MHz CD3OD); δ 13.54 (bs, 1H), 9.63 (s, 1H), 7.34 (s, 1H), 7.29 (d, 1H), 7.14-6.97 (m, 6H), 3.71 (t, 2H), 1.75 (qnt, 2H), 1.42 (sex, 2H), 0.95 (t, 2H); Mass Spectrum: M−H+ 439

1. customThe reaction mixture was evaporated
2. customthe residue was purified by flash chromatography