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

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.