关键词: 沙利度胺, 衍生物, 一步法, 合成

Abstract: 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.

Key words: Thalidomide, Derivatives, One-step method, Synthesis