【摘 要】
：
As a privileged scaffold,dibenzoazepine,a special type of heterocycles with two benzene rings fused to different positions of an azepine group,is used to derive pharmaceutical agents with various phar
【机 构】
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College of Chemistry & Chemical Engineering, Yangzhou University, Yangzhou 225002, China
【出 处】
：
中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
As a privileged scaffold,dibenzoazepine,a special type of heterocycles with two benzene rings fused to different positions of an azepine group,is used to derive pharmaceutical agents with various pharmacological properties.The synthetic way to build up the dibenzo[b,d]azepine skeleton would be necessary to accelerate or expand its applications in the drug discovery.When we attempted the multicomponent reaction of isatins,indan-1,3-dione and N-phenacylisoquinolinium salts to get the[3+2]cycloaddition product.a novel[4+1]adduct was achieved from double nucleophilic additions of indan-1,3-dione to the condensation product of isatins and N-phenacylisoquinolinium salts due to the strong electrophilic natures of C 1 carbon and carbonyl carbon of N-phenacylisoquinolinium salts.Thus,a unique two-carbon ring expansion of isatins has been achieved to conveniently construct the functionalized dibenzo[b,d]azepin-6-ones in moderate to high yield while one carbon is from N-substituent of pyridinium bromide and the other is from indene-1,3-dione.However,pyridinium bromide with less electron-withdrawing p-nitrobenzyl groupin in the reaction only resulted in a series of zwitterionic compounds.
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