A novel and practical method for the synthesis of dinotefuran through Michael addition of nitromethane to diethyl maleate

作者：Li, Haifeng; Wang, Lailai^*

来源：Tetrahedron, 2018, 74(2): 336-340.

DOI：10.1016/j.tet.2017.12.002

• Dinotefuran
• Synthesis
• Mickael addition
• Nitromethane
• Diethyl maleate

A novel and practical synthesis of dinotefuran 1, featuring a new access to it from known key intermediate (tetrahydrofuran-3-yl)-methanamine 5, has been achieved through Michael addition reaction of nitromethane to diethyl maleate in 6 steps with 45.5% total yield. This synthesis is scalable and hence has high potential for application to further synthetic elaboration on such new neonicotinoid insecticide dinotefuran 1.

• 出版日期2018-1-11
• 单位中国科学院兰州化学物理研究所; 羰基合成与选择氧化国家重点实验室