【摘 要】
：
Due to the significant bioactive properties of azepine moiety exhibited in many pharmaceuticals and natural products,1 many methods for the preparation of azepine-containing heterocycles have been dev
【机 构】
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武汉大学化学与分子科学学院 武汉430072 武汉大学化学与分子科学学院 武汉430072;南开大
【出 处】
：
中国化学会全国第十一届有机合成化学学术研讨会
论文部分内容阅读
Due to the significant bioactive properties of azepine moiety exhibited in many pharmaceuticals and natural products,1 many methods for the preparation of azepine-containing heterocycles have been developed.2 However, most of those methods require multiple-step synthesis.Therefore, the development of a general and facile [4 + 3]cycloaddition using common amine acid derived imine esters to access azepine frameworks remains highly desired.3Herein, we developed an unprecedented catalytic tandem formal [4 + 3] cycloaddition/decarboxylation/isomerization of methyl coumalate and imine esters (Scheme 1).This tandem reaction only requires Et3N as the mild base affording a series of highly functionalized seven-membered heterocyclic azepine derivatives in good yields with excellent regioselectivities.
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