Transition-metal-free highly regioselective C–H acetoxylation of pyrrolo[2,3-d]pyrimidine derivatives,Organic Chemistry Frontiers

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Transition-metal-free highly regioselective C–H acetoxylation of pyrrolo[2,3-d]pyrimidine derivatives
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020-08-12 , DOI: 10.1039/d0qo00702a
Zhengtong Mao _{1,

2,

3,

4} , Min Liu _{1,

2,

3,

4} , Gaoyang Zhu _{1,

2,

3,

4} , Jing Zhou _{1,

2,

3,

4} , Xingxian Zhang _{1,

2,

3,

4}

Affiliation

A simple and efficient methodology was developed for the direct C(sp²)–H acetoxylation of pyrrolo[2,3-d]pyrimidine derivatives. This highly regioselective one-pot acetoxylation was carried out under transition-metal-free conditions in the presence of NaI. This protocol provides a variety of acetoxylated pyrrolo[2,3-d]pyrimidines in good to excellent yields, which are potentially of great importance in medicinal chemistry. And this methodology was also proved to be practical by the gram-scale synthesis.

中文翻译：

吡咯并[2,3-d]嘧啶衍生物的无过渡金属的高区域选择性C–H乙酰氧基化

开发了一种简单有效的方法用于吡咯并[2,3- d ]嘧啶衍生物的直接C（sp ²）-H乙酰氧基化。这种高度区域选择性的一锅乙酰氧基化反应是在无过渡金属的NaI存在下进行的。该方案提供了各种乙酰氧基化的吡咯并[2,3- d ]嘧啶，收率良好至极佳，这在药物化学中可能具有重要意义。并通过克级合成证明了该方法的实用性。

更新日期：2020-09-16

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