A variety of furo[2,3-][1,4]diazepin-3-one derivatives were facilely synthesized through one-pot tandem cyclization/[4 + 3] annulation reactions between enynamides and α-bromohydroxamates. The reactions proceeded efficiently at room temperature, and various functional groups were well tolerated. The obtained furo[2,3-][1,4]diazepin-3(2)-ones containing a 7-membered dinitrogen-fused ring might be of biological and medicinal value.
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