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Synthesis of 11-14C-Quetiapine, 11-14C-Isoclotiapine and 10-(4-Methylpiperazin-1-Yl)Pyrido[4,3-B][1,4]Benzothiazepine[10-14C] Publisher



Saadatjoo N1 ; Javaheri M1, 2 ; Saemian N2 ; Amini M3
Authors
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Authors Affiliations
  1. 1. Department of Organic Chemistry, Faculty of Chemistry, Semnan University, PO Box: 35131-19111, Semnan, Iran
  2. 2. Applied Radiations Research School, Nuclear Science and Technology Research Institute, P.O.Box: 11365-3486, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy and Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran

Source: Journal of Radioanalytical and Nuclear Chemistry Published:2016


Abstract

Quetiapine is one of the most widely used antipsychotic drug which acts as an antagonist for multiple neurotransmitter receptor sites. 2-[2-(4-(Dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)ethoxy]ethanol (quetiapine) labeled with carbon-14 in 11-position has been synthesized as part of a 5-step sequence from anthranilic acid-[carboxy-14C]. We have presented a convenient synthetic pathway for labeling of quetiapine with carbon-14 by using one-pot procedures from a key thiazepin-11(10H)-one-[11-14C] by good radiochemical yield. And also isoclotiapine[11-14C], and 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine[10-14C], synthesized according to this route. © 2016, Akademiai Kiado, Budapest, Hungary.