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Organotin-catalyzed synthesis of hydroxyalkylamides from lactones via a ring-opening process
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2021-01-16 , DOI: 10.1016/j.tetlet.2021.152821
Xiayu Liang , Peng Yu , Chen Fu , Yongcun Shen

A new strategy for the facile synthesis of hydroxyalkylamides through the ring-opening reaction of lactone with amine promoted by dibutyltin acetate was developed. A series of hydroxyalkylamide compounds were obtained and the method was successfully applied to the synthesis of pharmaceutically active molecules tyrosinase inhibitor V and HDAC inhibitor VI via a three-step synthetic pathway. The broad substrate scope, mild reaction conditions and practical application proved the effectiveness, compatibility and practicality of this method.



中文翻译:

有机碳素通过开环过程从内酯催化合成羟烷基酰胺

提出了通过乙酸二丁锡促进内酯与胺的开环反应轻松合成羟烷基酰胺的新策略。获得了一系列羟烷基酰胺化合物,并将该方法成功地通过三步合成途径用于合成药物活性分子酪氨酸酶抑制剂V和HDAC抑制剂VI。广泛的底物范围,温和的反应条件和实际应用证明了该方法的有效性,兼容性和实用性。

更新日期:2021-02-26
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