2-苯基-3-(4,5,6-三甲基嘧啶-2-基)-2H-1,3-苯并噻嗪烷-4-酮的微波辐射合成

Synthesis of 2- phenyl- 3-( 4,5,6- trimethylpyrimidin- 2- yl)- 2H- [1,3]benzothiazin- 4- one under Microwave Irradiation

以苯甲醛、4,5,6-三甲基嘧啶-2-胺和硫代水杨酸为原料,以N,N’-二环己基碳二亚胺(DCC)/4-二甲氨基吡啶(DMAP)为催化剂,利用微波辐射的方法,三组分一锅法合成了2-苯基-3-(4,5,6-三甲基嘧啶-2-基)-2H-1,3-苯并噻嗪烷-4-酮。结果表明:n(苯甲醛)∶n(4,5,6-三甲基嘧啶-2-胺)∶n(硫代水杨酸)=1.2∶1.0∶2.0,2.0 equiv DCC,0.2 equiv DMAP,120℃,120 W,微波辐射10 min,收率达到76.3%。该反应具有操作简便、时间短、容易控制等优点。

2- phenyl- 3-（ 4,5,6- trimethylpyrimidin- 2- yl）- 2H- [1,3]benzothiazin- 4- one was synthesized with benzaldehyde,4,5,6- trimethylpyrimidin- 2- amin and thiosalicylic acid under microwave irradiation,in the presence of dicyclohexylcarbodiimide and 4- dimethylaminopyridine. The results showed that the target compound yield was 76. 3% under the optimum operation conditions： n（ benzaldehyde） ∶ n（ 4,5,6- trimethylpyrimidin- 2-amine） ∶n（ thiosalicylic acid） = 1. 2 ∶1. 0 ∶2. 0,2. 0 equiv DCC,0. 2 equiv DMAP,120 ℃,120 W,MW 10 min.The one- pot reaction had such advantages as simple procedure,short reaction time and easy control.