含有活性官能团的标题化合物是合成具有生物活性有机磷化合物的重要中间体,利用呋喃甲醛、噻吩甲醛和对氯苯甲醛与亚膦酸二乙酯在无溶剂条件下以三乙胺为催化剂简便地得到了标题化合物,产率74%~91%,并经元素分析、IR、^1HNMR、^13CNMR、MS确认了它们的化学结构。通过X射线单晶衍射测定了α-羟基-2'-噻吩甲基膦酸二乙酯和α-羟基-4'-氯代苄基膦酸二乙酯的晶体结构。
The dialkyl-hydroxy-hetero ( aryl ) cyclo-substituted phosphonates containing active groups are important intermediates for the synthesis of biologically active organophosphorus compounds. In this article, the organophosphorus compounds were easily prepared in 74% -91% yields by the reactions of 2-furaldehyde, 2-thiophenecarboxaldehyde or 4-chlorobezaldehyde, with diethyl hydrogen phosphite catalyzed by triethylamine in the absence of solvent. The compounds were identified on the basis of their elemental analysis and spectroscopic data, such as IR, ^1HNMR,^13CNMR and MS.The crystal structures of diethyl α-hydroxy-2-thiophenemethylphosphonate and diethyl α-hydroxy-4'-chlorobenzenemethyl-phosphonate were determined by the X-ray single crystal diffraction method.