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.
Microwave assisted formation of C-Te bonds is applied to the preparation of p-methoxyphenyltellurium trichloride in a fast, direct and simple way.Aryl chalcogenides structural motifs are commonly found in a variety of molecules with biological interest 1 and new materials 2 . Furthermore, organotellurium compounds have been used as precursors in the synthesis of molecules with different functionalities, such as dienes and enediynes, 3 present in the structure of important classes of natural products. 4
Ammonium trichloro [1,2-ethanediolato-O,O']-tellurate (AS101) is a potent immunomodulator with a variety of potential therapeutic applications. An easy, efficient and fast procedure for syntheses of AS101 by microwave-assisted organic synthesis is presented.
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