Tóm tắt

Objectives: To investigate the conditions for the synthesis of thalidomide in two-step with the assistance of microwave irradiation resulted in high overall yield. Method: Preparation of thalidomide which comprises reacting anhydride phthalic with L-glutamic acid to afford N-phthaloyl-DL-glutamic acid, which is further subjected to cyclization with ammonia donor sources (urea, ammonium acetate, thiourea) in presence of 4-dimethyl-aminopyridine and diphenyl either to give thalidomide. Results: Investigating the conditions of the reaction including temperature, duration and mode of reaction; ratio of reactive agents of preparation of thalidomide. From these results, we found out the conditions to synthesize this compound. Conclusion: An improved synthesis for thalidomide was established. It produced a total yield of 72% over two steps. * Keywords: Thalidomide; Phthalic acid; L-glutamic acid; Synthesis.

Abstract

Objectives: To investigate the conditions for the synthesis of thalidomide in two-step with the assistance of microwave irradiation resulted in high overall yield. Method: Preparation of thalidomide which comprises reacting anhydride phthalic with L-glutamic acid to afford N-phthaloyl-DL-glutamic acid, which is further subjected to cyclization with ammonia donor sources (urea, ammonium acetate, thiourea) in presence of 4-dimethyl-aminopyridine and diphenyl either to give thalidomide. Results: Investigating the conditions of the reaction including temperature, duration and mode of reaction; ratio of reactive agents of preparation of thalidomide. From these results, we found out the conditions to synthesize this compound. Conclusion: An improved synthesis for thalidomide was established. It produced a total yield of 72% over two steps. * Keywords: Thalidomide; Phthalic acid; L-glutamic acid; Synthesis.