一种通过一锅法偶联-异构化-环缩合序列合成新型1,5-苯并杂氮杂卓的方法。
A novel 1,5-benzoheteroazepine synthesis via a one-Pot coupling-isomerization-cyclocondensation sequence.
作者信息
Braun RU, Zeitler K, Muller TJ
机构信息
Department Chemie, Ludwig-Maximilians-Universitat Munchen, Butenandtstr. 5-13 (Haus F), D-81377 Munchen, Germany.
出版信息
Org Lett. 2000 Dec 28;2(26):4181-4. doi: 10.1021/ol006721k.
2,4-Di(hetero)aryl substituted 2,3-dihydro 1,5-benzoheteroazepines (hetero = NH, O, S) can be readily sythesized in a one-pot process initiated by a coupling-isomerization sequence of an electron poor (hetero)aryl halide and a terminal propargyl alcohol subsequently followed by a cyclocondensation with 2-amino, 2-hydroxy, or 2-mercapto anilines. In addition, the structures were established unambiguously by an X-ray structure analysis of 7a.
2,4-二（杂）芳基取代的2,3-二氢-1,5-苯并杂氮杂卓（杂 = NH、O、S）可以通过贫电子（杂）芳基卤化物与末端炔丙醇的偶联-异构化序列引发的一锅法轻松合成，随后与2-氨基、2-羟基或2-巯基苯胺进行环缩合。此外，通过对7a的X射线结构分析明确确定了结构。
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