A Ring Expansion Route to Benzofused N‐Heterocycles Through Aryne Insertion into 1,3‐Diaza‐heterocycles
作者:Yun Yang、Yue Xu、Christopher R. Jones
DOI:10.1002/ejoc.201900570
日期:2019.9
Ring expansion of 1,3‐diaza‐heterocycles is reported for the synthesis of benzofused N‐heterocycles, which operates via the first examples of formal aryne insertion into a C(sp3)–N σ‐bond. 2,3,4,5‐Tetrahydro‐1H‐benzo[e][1,4]diazepines and 1,2,3,4‐tetrahydroquinazolines have been prepared from the corresponding imidazolidines and 1,3‐diazetidines.
据报道,苯并稠合的N-杂环的合成具有1,3-二氮杂杂环的扩环作用,该过程通过将芳烃正式插入C(sp3)-Nσ-键的第一个例子进行。由相应的咪唑烷和1,3-二氮杂啶制备了2,3,4,5-四氢-1H-苯并[ e ] [1,4]二氮杂和1,2,3,4-四氢喹唑啉。