Zheng Yongpeng, Li Jianxiao, Qi Chaorong, Wu Wanqing, Jiang Huanfeng
Key Laboratory of Functional Molecular Engineering of Guangdong Province, School of Chemistry and Chemical Engineering, South China University of Technology, Guangzhou 510641, China.
J Org Chem. 2024 Oct 18;89(20):15289-15301. doi: 10.1021/acs.joc.4c01010. Epub 2024 Oct 4.
Herein, a base-promoted strategy for the synthesis of β-amino acids derivatives from α,β-unsaturated acyl chlorides derivatives and aryl amines has been described. In the presence of triethylamine, a tandem Michael addition and nucleophilic substitution progress was generated. The current method features readily available raw materials, mild reaction conditions, high atom economy, and wide tolerance for the coupling partners.
在此，已描述了一种由α,β-不饱和酰氯衍生物和芳基胺合成β-氨基酸衍生物的碱促进策略。在三乙胺存在下，发生了串联迈克尔加成和亲核取代反应。该方法具有原料易得、反应条件温和、原子经济性高以及对偶联伙伴耐受性广的特点。
