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目前应用的多种抗病毒药均属核苷类抗代谢药物,而膦羧酸化合物膦乙酸双钠(Ⅳ)及膦甲酸钠(Ⅸ)虽非抗代谢药物,但具有显著的抗病毒活性;且后者因无骨髓累积毒性等副作用而优于前者有关膦羧酸化合物的合成早有报道,其方法主要是应用Arbuzov反应将卤代酸酯与亚磷酸三乙酯缩合,然后在封管中水解而得;也可将亚磷酸二乙酯先与金属钠制成钠盐,再与卤代酸酯缩合、水解制得。我们系采用下列路线合成膦乙酸双钠及膦乙酸正丙酯双钠。
A variety of antiviral drugs currently used are nucleoside antimetabolites. Phosphine carboxylic acid compounds, phosphonoacetic acid disodium (Ⅳ) and foscarnet (Ⅸ), have significant antiviral activity, though not antimetabolites; and The latter due to no side effects such as accumulation of toxicity and bone marrow is superior to the former synthesis of phosphonic acid compounds have long been reported, the method is mainly Arbuzov reaction of halogenated esters and triethyl phosphite condensation, and then sealed in the tube hydrolysis Derived; also sodium phosphite can be made with the first sodium sodium salt, and then halogenated acid ester condensation, hydrolysis obtained. We use the following route to synthesize disodium phosphoacetate and n-propyl phosphite.