9芴酮的简易还原氨化
On Facile Reductive Amination of 9-Fluorenone
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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．Abstract: 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 .
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