1,3-二氢-1,3-二酮-2-氢-异吲哚衍生物的合成研究  

Synthesis of 1,3-Dihydro-1,3-dioxo-2H-isoindole Derivatives

作　　者：杨跃[1] 向东[1] 郭举[1] 郑永胜[1] 叶斌[2] 杨金亮[3] 成丽[4] 

机构地区：[1]四川大学华西药学院药物化学教研室,成都610041 [2]四川省第六人民医院 [3]四川大学华西医院人类疾病生物治疗国家重点实验室肿瘤中心 [4]四川大学华西药学院现代药学专业教学中心室

出　　处：《四川大学学报（医学版）》2008年第4期645-647,共3页Journal of Sichuan University(Medical Sciences)

摘　　要：目的设计并合成沙利度胺的衍生物。方法氨基酸苄酯氨解N-邻苯二甲酰基-L-谷氨酸酐,所得产物经氢化脱苄后再与氨气成铵盐即得1,3-二氢-1,3-二酮-2H-异吲哚衍生物。结果成功地合成了4个未见文献报道的沙利度胺衍生物。并进行了结构表征。结论利用本方法可以在温和的条件下获得较高产率的目标产物。Objective To synthesize a series of derivatives of Thalidomide.Methods The N-Phthaloyl-L-glutamic anhydride was ammonolyzed with amino acid benzyl esters,followed by hydrogenization.The reaction between the hydogenized products and ammonia gas produced ammonium salt,1,3-dihydro-1,3-dioxo-2H-isoindole derivatives.Results Four new derivatives of Thalidomide were obtained and confirmed by spectral detection.Conclusion The derivatives of Thalidomide can be efficiently synthesized under mild conditions.

关 键 词：沙利度胺 合成 1 3-二氢-1 3-二酮-2-氢-异吲哚衍生物 血管生成 

分 类 号：R914.5[医药卫生—药物化学]