Novel Microwave-Assisted Synthesis of the Immunomodulator Organotellurium Compound Ammonium Trichloro(dioxoethylene-O,O')tellurate (AS101)

International Journal of Molecular Sciences

M. Pilar Vázquez-Tato¹  Alberto Mena-Menéndez¹  Xesús Feás¹ 

[1] Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain;

关键词: Tellurium;    AS101;    ammonium trichloro[1;    2-ethanediolato-O;    O′]-tellurate;    microwave irradiation;    antitumoral;   

DOI  :  10.3390/ijms15023287

来源: mdpi

【 摘 要 】

Ammonium trichloro[1,2-ethanediolato-O,O′]-tellurate (AS101) is the most important synthetic Te compound from the standpoint of its biological activity. It is a potent immunomodulator with a variety of potential therapeutic applications and antitumoral action in several preclinical and clinical studies. An experimental design has been used to develop and optimize a novel microwave-assisted synthesis (MAOS) of the AS101. In comparison to the results observed in the literature, refluxing Te(IV) chloride and ethylene glycol in acetonitrile (Method A), or by refluxing Te(IV) chloride and ammonium chloride in ethylene glycol (Method B), it was found that the developed methods in the present work are an effective alternative, because although performance slightly decreases compared to conventional procedures (75% vs. 79% by Method A, and 45% vs. 51% by Method B), reaction times decreased from 4 h to 30 min and from 4 h to 10 min, by Methods A and B respectively. MAOS is proving to be of value in the rapid synthesis of compounds with new and improved biological activities, specially based on the benefit of its shorter reaction times.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland