劳森试剂促进了恶唑酮的脱氧反应以用于2,4-二取代噻唑的合成。

Lawesson's reagent promoted deoxygenation of azlactones for the syntheses of 2,4-disubstituted thiazoles.

作者信息

Yin Gaofeng, Wang Xiaodong, Wang Yuqing, Shi Tao, Zeng Yaofu, Wang Yuying, Peng Xue, Wang Zhen

机构信息

School of Pharmacy, Lanzhou University, West Donggang Road. No. 199, Lanzhou 730000, China.

School of Pharmaceutical Science, Hengyang Medical School, University of South China, West Changsheng Road. No. 28, Hengyang 421001, China.

出版信息

Org Biomol Chem. 2022 Dec 14;20(48):9589-9592. doi: 10.1039/d2ob01939f.

DOI:10.1039/d2ob01939f

PMID:36408836

Abstract

Azlactones and thiazoles are common structural motifs and possess diverse applications. A new method for the efficient and straightforward syntheses of 2,4-disubstituted thiazoles from azlactones has been developed. The reaction proceeded deoxygenation of azlactones by Lawesson's reagent without metal or external additives. A variety of 2,4-disubstituted thiazoles were synthesized with up to 92% yield. Furthermore, the importance of this methodology was also justified by a gram-scale synthesis.

摘要

氮杂内酯和噻唑是常见的结构基序，具有多种应用。已开发出一种从氮杂内酯高效直接合成2,4-二取代噻唑的新方法。该反应通过劳森试剂使氮杂内酯脱氧，无需金属或外部添加剂。合成了多种2,4-二取代噻唑，产率高达92%。此外，克级规模的合成也证明了该方法的重要性。