西南师范大学学报(自然科学版)
西南師範大學學報(自然科學版)
서남사범대학학보(자연과학판)
JOURNAL OF SOUTHWEST CHINA NORMAL UNIVERSITY
2014年
9期
26-29
,共4页
夏科学%熊阳%杨大成%范莉
夏科學%熊暘%楊大成%範莉
하과학%웅양%양대성%범리
9-芴酮%9-芴酮肟%9-芴胺%还原氨化
9-芴酮%9-芴酮肟%9-芴胺%還原氨化
9-물동%9-물동우%9-물알%환원안화
9-Fluorenone%9-Fluorenone oxime%9H-Fluoren-9-amine%Reductive Amination
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芴基結構單元是重要的多功能中間體和生物活性片段,9芴基的官能化在藥物分子轉換方麵具有重要意義.報道瞭9芴酮還原氨化的實用方法.9芴酮與鹽痠羥胺反應得9芴酮肟,9芴酮肟經多種還原劑還原為9芴胺.通過條件優化,高收率(高于95%)得到9芴肟,中等收率(鋅粉還原法)製得9芴胺,從而髮現瞭未見文獻報道的9芴酮肟及9芴胺閤成的簡便操作方法.
9물기결구단원시중요적다공능중간체화생물활성편단,9물기적관능화재약물분자전환방면구유중요의의.보도료9물동환원안화적실용방법.9물동여염산간알반응득9물동우,9물동우경다충환원제환원위9물알.통과조건우화,고수솔(고우95%)득도9물우,중등수솔(자분환원법)제득9물알,종이발현료미견문헌보도적9물동우급9물알합성적간편조작방법.
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 .