铜催化烷基磷酸酯与醇或醚的偶联反应及核苷类氢亚磷酸酯的合成研究
Copper-Catalyzed Coupling Between H-Phosnonate and Alcohols or Ethers and the Study on Synthesis of Nucleoside H-Phosphonates Derivatives
Abstract
α-羟基膦酸酯具有多种生物活性,例如,抗菌、抗病毒、抗HIV、植物生长调节剂及酶的抑制剂,在天花、高血压、恶性肿瘤及HIV疾病治疗方面具有良好前景。该类化合物的常用合成方法是Pudovik反应或Abramov反应,通过氢亚磷酸酯或三配位的磷试剂与醛酮反应制备;还有一些是基于膦酸酯类衍生物,如烷基膦酸酯的氧化,α-羰基膦酸酯化合物的还原或加成反应来合成α-羟基膦酸酯。近年来发展了一批金属或无金属催化醇或醚与亲核试剂构建C-C或C-X(OorN)键的反应;尽管很多杂原子可以作为亲核试剂与醇或醚反应,但氢亚磷酸酯与该类化合物来制备α-羟基膦酸酯的反应却未见报道。 本论文以CuCl2为催化剂,在过氧... α-Hydroxy phosphonates have attracted considerable attention owing to their critical roles in several fields. They showed potential biological activities, such as antibacterial, antiviral, anticancer drugs, plant growth regulators and enzyme inhibitor properties which widely used in the treatment of smallpox, hypertension, malignancy, and HIV disease. The traditional way to synthesize α-hydroxy ph...