title: Novel microwave-assisted synthesis of the immunomodulator organotellurium compound ammonium trichloro(dioxoethylene-O,O')tellurate (AS101).
abstract: 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.
authors.affiliation: Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain. pilar.vazquez.tato@usc.es.
authors.forename: M Pilar
authors.initials: MP
authors.lastname: Vázquez-Tato
authors.affiliation: Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain. menamenendez@hotmail.es.
authors.forename: Alberto
authors.initials: A
authors.lastname: Mena-Menéndez
authors.affiliation: Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain. xesus.feas@usc.es.
authors.forename: Xesús
authors.initials: X
authors.lastname: Feás
authors.affiliation: Department of Organic Chemistry, Faculty of Science, University of Santiago de Compostela, E-27002 Lugo, Spain. julioa.seijas@usc.es.
authors.forename: Julio A
authors.initials: JA
authors.lastname: Seijas
mesh_terms: D015195:Drug Design; D005030:Ethylenes / Q000138:chemical synthesis* / Q000737:chemistry; D007155:Immunologic Factors / Q000138:chemical synthesis* / Q000737:chemistry; D008872:Microwaves
chemical_list: D005030:Ethylenes; D007155:Immunologic Factors; C054105:ammonium trichloro(dioxoethylene-O,O'-)tellurate