Ugi反应脱Boc保护基环合策略在含氮杂环合成中的应用

Application of Ugi/De-Boc/Cyclization Strategy in the Synthesis of Nitrogen-Containing Heterocycles

Ugi反应脱Boc保护基环合(UDC)策略是一种"三步一锅煮法",采用带Boc保护氨基的双官能团底物参与Ugi多组分反应,随后在酸性条件下脱去保护基并环合得到含氮杂环化合物.该策略具有快速、高效、经济和结构多样性的特点,可用于构建复杂含氮杂环化合物库,近来受到广泛关注.对近年来UDC策略在合成五元、六元、七元杂环和天然产物方面应用的研究进展进行了综述.

Ugi/de-Boc/cyclization（UDC） strategy represents a ＂three-step, one-pot procedure＂, employing the Ugi multicomponent reaction utilizing one bi-functional group substrates with N-Boc-protected amino, followed by Boc-deprotection and cyclization to synthesize nitrogen-containing heterocycles. This strategy has the characteristics of rapid, efficiency, economy and structural diversity, which can be used to build libraries of complex nitrogen-containing heterocycles and has drawn much attention recently. In this paper, the research progress of UDC strategy in the synthesis of five-, six- and seven-membered heterocycles and natural products were summarized.