4-(4-氯苯基)-3-甲基-2,4-二氧代丁酸乙酯的合成

Synthesis of Ethyl 4-(4-Chlorophenyl)-3-methyl-2,4-dioxobutyrate

对氯苯丙酮经烯胺化得4-[(Z)-1-(4-氯苯基)丙烯基]吗啉,再与草酰氯单乙酯缩合得利莫那班合成中间体4-(4-氯苯基)-3-甲基-2,4-二氧代丁酸乙酯,纯度91%,粗收率66%。

Ethyl 4-（4-chlorophenyl）-3-methyl-2,4-dioxobutyrate, an intermediate of antiobesity agent rimonabant was synthesized from p-chloropropiophenone by enamination to give 4-[ （Z）- 1-（4- chlorophenyl） propenyl] morpholine, followed by condensation with chlorooxalic acid ethyl ester in 66 % crude yield.