Copper-Catalyzed Synthesis of Medium- and Large-Sized Nitrogen Heterocycles via N-Arylation of Phosphoramidates and Carbamates
作者:Ting Yang、Changxue Lin、Hua Fu、Yuyang Jiang、Yufen Zhao
DOI:10.1021/ol052126c
日期:2005.10.1
[reaction: see text] We have developed an efficient method for the preparation of medium- and large-sized nitrogen heterocycles via copper-catalyzed intramolecular N-arylation of phosphoramidates and carbamates. Introduction of the phosphoryl group or tert-butoxycarbonyl at N-termini can improve intramolecular cyclization under copper catalysis, and the phosphoryl and tert-butoxycarbonyl can easily
[反应:见正文]我们已经开发了一种通过铜催化的氨基磷酸酯和氨基甲酸酯的分子内N-芳基化反应制备中型和大型氮杂环的有效方法。在N-末端引入磷酰基或叔丁氧羰基可以改善铜催化下的分子内环化,并且在温和的条件下可以容易地除去磷酰基和叔丁氧羰基。因此,该方便有效的方法适用于中,大型氮杂环的制备。