一步法合成沙利度胺及其重要的衍生物  被引量:5

One-step Synthesis of Thalidomide and Its Important Derivatives

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作  者:袁修华[1] 郭海泉[1] 邱雪鹏[1] 康传清[1] 刘旭东[1] 高连勋[1] 

机构地区:[1]中国科学院长春应用化学研究所高分子工程研究室,中国科学院研究生院长春130022

出  处:《高等学校化学学报》2005年第8期1477-1479,共3页Chemical Journal of Chinese Universities

摘  要:Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2—5 directly in yields 24%47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and Lglutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2-5 directly in yields 24 %-47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.

关 键 词:沙利度胺 衍生物 一步法 合成 

分 类 号:O621[理学—有机化学]

 

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