反应详情

Analogues to the sulfonylurea formation described in Ex. 5, 3-(4-aminophenyl)-6-chloro-7-(methylamino)-2,3-dihydrobenzo[e][1,3]oxazin-4-one (Ex. 47) (44 mg, 0.15 mmol) and (5-Chloro-thiophene-2-sulfonyl)-carbamic acid ethyl ester (59 mg, 0.22 mmol) were coupled to give 1-(5-chlorothiophen-2-ylsulfonyl)-3-(4-(6-chloro-7-(methylamino)-4-oxo-2H-benzo[e][1,3]oxazin-3(4H)-yl)phenyl)urea. RP-HPLC: 2.70 min; ES-MS (M+H)+=528.0; 1H-NMR (MeOH-d4) δ (ppm): 2.8 (s, 3), 5.4 (s, 2), 6.2 (s, 1), 6.9 (d, 1), 7.1 (d, 2), 7.39 (d, 1), 7.48 (d, 2), 7.7 (s, 1).