1-Alkenylphosphonic acid derivatives of purines have been proven to exhibit significant antiviral activity among these series of compounds. Here we disclose the stereoselective synthesis of the constrained analogs of 1-alkenylphosphonate derivatives of purines via intramolecular epoxide opening reaction of γ,δ-epoxyalkanephosphonates with subsequent Mitsunobu coupling reactions with purine bases.
嘌呤的1-烯基
膦酸衍
生物已被证明在这些系列化合物中显示出显着的抗病毒活性。在这里,我们公开了通过γ,δ-环氧烷
膦酸酯的分子内
环氧化物开环反应以及随后的与
嘌呤碱基的Mitsunobu偶联反应的
嘌呤的1-烯基
膦酸酯衍
生物的受约束类似物的立体选择性合成。