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Probing the Reactivity of 2,4-Dichlorofuro[3,4-d]pyrimidin-7-one: A Versatile and Underexploited Scaffold to Generate Substituted or Fused Pyrimidine Derivatives
Synlett ( IF 1.7 ) Pub Date : 2019-09-24 , DOI: 10.1055/s-0039-1690205
Paolo Vincetti , Gabriele Costantino , Maria Grazia Martina , Marco Radi

Herein, we describe the results of our investigation on the chemical reactivity and versatility of a poorly explored scaffold: 2,4-dichlorofuro[3,4-d]pyrimidin-7-one (3). Highly functionalized pyrimidines can be obtained with a divergent approach by reacting the key intermediate 3 with different amine nucleophiles under carefully controlled reaction conditions. The set-up of a microwave-assisted one-pot, two- or three-step protocol to rapidly generate 2,4,5,6-tetrasubstituted or fused pyrimidines is also reported.

中文翻译:

探索 2,4-二氯呋喃 [3,4-d]pyrimidin-7-one 的反应性:用于生成取代或融合的嘧啶衍生物的多功能且未充分利用的支架

在此,我们描述了我们对研究不足的支架的化学反应性和多功能性的调查结果:2,4-二氯呋喃 [3,4-d]pyrimidin-7-one (3)。通过将关键中间体 3 与不同的胺亲核试剂在仔细控制的反应条件下反应,可以采用不同的方法获得高度官能化的嘧啶。还报告了建立微波辅助一锅、两步或三步协议以快速生成 2,4,5,6-四取代或融合嘧啶。
更新日期:2019-09-24
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