developed to construct the highly fused indano[1,2-b]azirine frameworks in good yields with a broad range of substrates under mild reaction conditions. More intriguingly, a [4+1+1] sequential annulation cascade is demonstrated for the first time in this reaction and opened a new reaction mode for α-keto oximes. These fused indano[1,2-b]azirinederivatives could also be further transformed into intriguing
开发了 Rh(III) 催化的 α-酮肟的 C-H 活化和与重氮化合物的环化级联反应,以良好的产率构建高度稠合的茚满并[1,2- b ] 氮杂环丙烷骨架,并具有广泛的底物范围反应条件温和。更有趣的是,在该反应中首次证明了[4+1+1]顺序环化级联反应,并为α-酮肟开辟了新的反应模式。这些融合的茚满并[1,2- b ]氮丙啶衍生物也可以进一步转化为有趣的特权药物支架。
C–C Bond Cleavage-Induced C- to N-Acyl Transfer for Synthesis of Amides
作者:Su Eun Lee、Youngsoo Kim、Yong Ho Lee、Hee Nam Lim
DOI:10.1021/acs.orglett.4c01154
日期:2024.5.3
A new approach for the preparation of amides was developed using C–C bond cleavage that initiates C- to N-acyl transfer, employing activated ketones as acylation reagents and amine nucleophiles. The reaction was operational under the coupling reagent system that is commonly utilized for peptide bond formations. The method enables practical preparation of amides using linear and cyclic ketone substrates