反应详情

A solution of 2-Amino-4-(4-chloro-phenyl)-thiophene-3-carboxylic acid ethyl ester (4a) (1.759 g, 6.24 mmol) in diethyl malonate (8.0 g, 50 mmol) was heated at 180° C. for 4 hours. The excess diethyl malonate was removed under reduced pressure to give the title compound. MS (DCI/NH3) m/e 396 (M+H)+; 1H NMR (300 MHz, CDCl3): δ ppm 12.21 (s, 1H), 7.33–7.20 (m, 5H), 6.62 (s, 1H), 4.31 (q, J=7.12, 2H), 4.15 (q, J=7.12, 2H), 3.61 (s, 2H), 1.33 (t, J=7.12, 3H), 0.99 (t, J=7.12, 3H).

1. customThe excess diethyl malonate was removed under reduced pressure