4-二甲氨基吡啶促进的一锅法合成高选择性螺环丙烷吡唑啉酮衍生物
收稿日期: 2019-04-10
网络出版日期: 2019-07-09
基金资助
国家自然科学基金(21961038);国家自然科学基金(21462041)
High-Selective One-Pot Synthesis of Spirocyclopropane Pyrazolones Promoted by 4-Dimethylaminopyridine
Received date: 2019-04-10
Online published: 2019-07-09
Supported by
the National Natural Science Foundation of Chin(21961038);the National Natural Science Foundation of Chin(21462041)
发展了一种4-二甲氨基吡啶(DMAP)促进的高立体选择性合成多取代螺环丙烷吡唑啉酮的方法.该反应以吡唑啉酮、芳醛和溴乙酸酯为原料,DMAP作为碱,经三组分一锅反应,合成一系列收率高且非对映选择性好的目标化合物.该反应具有操作简单、产率高以及非对映选择性好等优点.该合成方法对于螺环丙烷的研究具有重要的价值.
关键词: 一锅法合成; 多组分反应; 螺环丙烷; 吡唑酮; 4-二甲氨基吡啶(DMAP)
梁杰 , 马会芳 , 阿布拉江·克依木 . 4-二甲氨基吡啶促进的一锅法合成高选择性螺环丙烷吡唑啉酮衍生物[J]. 有机化学, 2019 , 39(11) : 3169 -3175 . DOI: 10.6023/cjoc201904028
A 4-dimethylaminopyridine (DMAP)-promoted high stereoselectivity method for the synthesis of polysubstituted spiropropane pyrazolone was developed. A series of target compounds were synthesized from using pyrazolone, aromatic aldehyde and bromoacetate as raw materials, and DMAP as a base with high yield via three-component one-pot reaction. This reaction has the advantages of simple operation, high yield and good diastereotopic selectivity. In addition, this synthetic method is of great value for the study of spiropropane.
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