[Synthesis of 1,3-dihydro-1,3-dioxo-2H-isoindole derivatives].

Sichuan Da Xue Xue Bao Yi Xue Ban

The Central Teaching Laboratory for Modern Pharmacy, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

Published: July 2008

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.

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