Stereoselective synthesis of trans-aziridines via intramolecular oxidative C(sp3)–H amination of β-amino ketones,Organic Chemistry Frontiers

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Stereoselective synthesis of trans-aziridines via intramolecular oxidative C(sp3)–H amination of β-amino ketones
Organic Chemistry Frontiers ( IF 4.6 ) Pub Date : 2020/02/04 , DOI: 10.1039/c9qo01489f
Chen Tan _{1,

2,

3,

4,

5} , Yongguo Liu _{5,

6,

7,

8} , Xinyuan Liu _{1,

2,

3,

4,

5} , Huanxin Jia _{1,

2,

3,

4,

5} , Kun Xu _{5,

9,

10,

11} , Sihan Huang _{1,

2,

3,

4,

5} , Jingwen Wang _{1,

2,

3,

4,

5} , Jiajing Tan _{1,

2,

3,

4,

5}

Affiliation

Aziridines are ubiquitous in bioactive molecules and often serve as key synthetic building blocks. We report herein an intramolecular KI/TBHP mediated oxidative dehydrogenative C(sp³)–H amination reaction to synthesize a diverse array of trans-2,3-disubstituted aziridines in good yields under mild conditions. The synthetic utility of this protocol was further highlighted by a one-pot, two-step synthesis of unprotected aziridines.

中文翻译：

通过分子内β-氨基酮的氧化C（sp3）–H氨基化立体选择性合成反式氮丙啶

氮丙啶在生物活性分子中无处不在，通常用作关键的合成构件。我们在这里报告分子内KI / TBHP介导的氧化脱氢C（sp ³）-H胺化反应，以在温和的条件下以高收率合成各种不同的反式-2,3-二取代氮丙啶阵列。该方案的合成实用性通过未保护的氮丙啶的一锅两步合成得到了进一步强调。

更新日期：2020-03-03

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