Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines,Organic Chemistry Frontiers

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Sulfur-directed palladium-catalyzed C(sp3)–H α-arylation of 3-pyrrolines: easy access to diverse polysubstituted pyrrolidines
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020/01/20 , DOI: 10.1039/c9qo01440c
Guangwu Sun _{1,

2,

3,

4} , Xi Zou _{1,

2,

3,

4} , Jinping Wang _{1,

2,

3,

4} , Wen Yang _{1,

2,

3,

4}

Affiliation

A sulfur-directed palladium-catalyzed C(sp³)–H α-arylation of 3-pyrrolines has been disclosed by installing a thioacyl group as the directing group. The arylation reactions using arylboronic acids as coupling partners provided a variety of 2-aryl-3-pyrolines in moderate to good yields. Moreover, the α-arylated products were readily converted to various synthetically useful 3-pyrroline and pyrrolidine derivatives, especially polysubstituted pyrrolidines.

中文翻译：

硫导向的钯催化的3-吡咯啉的C（sp3）–Hα-芳基化：易于获得各种多取代的吡咯烷

通过安装硫酰基作为导向基团，已经公开了3-吡咯啉的硫定向钯催化的C（sp ³）-Hα-芳基化反应。使用芳基硼酸作为偶联伙伴的芳基化反应以中等至良好的产率提供了各种2-芳基-3-吡咯啉。此外，α-芳基化产物容易转化为各种合成上有用的3-吡咯啉和吡咯烷衍生物，特别是多取代的吡咯烷。

更新日期：2020-02-18

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