One-step Synthesis of Thalidomide and Its Important Derivatives

Abstract

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

CLC Number:

O621

TrendMD:

YUAN Xiu-Hua, GUO Hai-Quan, QIU Xue-Peng, KANG Chuan-Qing, LIU Xu-Dong, GAO Lian-Xun . One-step Synthesis of Thalidomide and Its Important Derivatives[J]. Chem. J. Chinese Universities, 2005, 26(8): 1477.

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One-step Synthesis of Thalidomide and Its Important Derivatives

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