The development of a versatile solid phase synthesis of bicyclic polyaza heterocycles including pteridines, purines, and deazapurines is described. The strategy comprises the linking of a pre-formed pyrimidine through a thioether at the 2 or 4 position to a polystyrene resin, the cyclisation of the second ring, and the direct or oxidative cleavage of the product from the resin by nucleophilic substitution
描述了包括蝶啶,
嘌呤和脱氮
嘌呤的双环多氮杂杂环的通用固相合成的开发。该策略包括将预先形成的
嘧啶通过2或4位的
硫醚连接至聚
苯乙烯树脂,第二环的环化以及通过亲核取代将产物从
树脂中直接或氧化裂解。这不仅提供了第二个环中取代基的变化,还提供了切割位点的变化。该方法范围的局限性是由
嘧啶基2-或4-
硫醚的固有反应性决定的,尽管它们在C5处容易硝化,却难以烷基化和酰化。