The treatment of F-alkyl ketones with sodium diethyl phosphite in tetrahydrofuran at −10 to 0 °C gave high yields of 1-substituted F-1-alkenyl phosphates, which readily reacted with amidine or hydrazine derivatives at room temperature to afford the corresponding fluorinated pyrimidines or pyrazoles, respectively, in good to excellent yields.
在
四氢呋喃中在 -10 至 0 °C 下用
二乙基亚磷酸钠处理 F-烷基酮,得到高产率的 1-取代 F-1-烯基
磷酸酯,其在室温下容易与脒或
肼衍
生物反应,得到相应的
氟化物。
嘧啶类或
吡唑类,分别具有良好到极好的产率。