摘要
9-芴基结构单元是重要的多功能中间体和生物活性片段,9-芴基的官能化在药物分子转换方面具有重要意义.报道了9-芴酮还原氨化的实用方法.9-芴酮与盐酸羟胺反应得9-芴酮肟,9-芴酮肟经多种还原剂还原为9-芴胺.通过条件优化,高收率(高于95%)得到9-芴肟,中等收率(锌粉还原法)制得9-芴胺,从而发现了未见文献报道的9-芴酮肟及9-芴胺合成的简便操作方法.
9-Fluorenyl structural unit is fundamental intermediates and essential biologically active frag-ment ,and the functionalization of 9-Fluorenyl is crucial in the drug molecule conversion .Herein a practical method of reductive amination of 9-fluorenone has been reported in this paper .A high yield conversion (〉95% ) has been achieved from 9-fluorenone to 9-fluorenone oxime under optimal condition ;furthermore , 9H-Fluoren-9-amine has been obtained by Zn reduction process with a medium yield for the first time , which is much better than reported in literature .This novel method provides a useful synthetic procedure with simple operation and low cost ,which also exhibits high commercial value .
出处
《西南师范大学学报(自然科学版)》
CAS
CSCD
北大核心
2014年第9期26-29,共4页
Journal of Southwest China Normal University(Natural Science Edition)
基金
国家级大学生创新训练项目(201310635036)
关键词
9-芴酮
9-芴酮肟
9-芴胺
还原氨化
9-Fluorenone
9-Fluorenone oxime
9H-Fluoren-9-amine
Reductive Amination