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1,3-二氢-1,3-二酮-2-氢-异吲哚衍生物的合成研究
引用本文:杨跃,向东,郭举,郑永胜,叶斌,杨金亮,成丽. 1,3-二氢-1,3-二酮-2-氢-异吲哚衍生物的合成研究[J]. 四川大学学报(医学版), 2008, 39(4): 645-647
作者姓名:杨跃  向东  郭举  郑永胜  叶斌  杨金亮  成丽
作者单位:四川大学华西药学院药物化学教研室,成都,610041;四川省第六人民医院;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;四川大学华西药学院现代药学专业教学中心室
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。

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

Synthesis of 1,3-Dihydro-1,3-dioxo-2H-isoindole Derivatives
YANG Yue,XIANG Dong,GUO Ju,ZHENG Yong-sheng,YE Bin,YANG din-liang,CHENG Li. Synthesis of 1,3-Dihydro-1,3-dioxo-2H-isoindole Derivatives[J]. Journal of Sichuan University. Medical science edition, 2008, 39(4): 645-647
Authors:YANG Yue  XIANG Dong  GUO Ju  ZHENG Yong-sheng  YE Bin  YANG din-liang  CHENG Li
Affiliation:The Central Teaching Laboratory for Modern Pharmacy, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Abstract:
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.
Keywords:Thalidomide synthesis 1  3-dhydro-1  3-dioxo-2H-isoindole derivatives Angiogenesis
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