Reactivity of the ester group attached isoxazoline, benzisoxazole, and isoxazole: a facial preparation of 3-acyl-substituted these heterocycles
作者:Kenichi Murai、Shuji Miyazaki、Hiromichi Fujioka
DOI:10.1016/j.tetlet.2012.05.006
日期:2012.7
A facile preparation of 3-acyl-substituted isoxazolines, benzisoxazoles, and isoxazoles from the corresponding 3-carboxylate esters is described. The process, involving reaction of the ester derivative of 3-carboxylic acid substituted heterocycles with Grignard or alkynyl lithium reagents, leads to direct generation of the corresponding 3-acyl heterocycle. The presence of α-imino ester moieties in
描述了由相应的3-羧酸酯容易地制备3-酰基取代的异恶唑啉,苯并异恶唑和异恶唑的方法。该方法涉及3-羧酸取代的杂环的酯衍生物与格氏试剂或炔基锂试剂的反应,导致直接生成相应的3-酰基杂环。在杂环底物中用于反应的α-亚氨基酯部分的存在被认为是控制这些转化性质的关键特征。该新方法的合成效用通过在两步法中制备新型连接双杂环的应用得到了证明。