Synthesis of 11-14C-quetiapine, 11-14C-isoclotiapine and 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine[10-14C]

被引：0
|
作者：
Saadatjoo, Naghi [1 ]
Javaheri, Mohsen [1 ,2 ]
Saemian, Nader [2 ]
Amini, Mohsen [3 ,4 ]
机构：
[1] Semnan Univ, Dept Organ Chem, Fac Chem, POB 35131-19111, Semnan, Iran
[2] Nucl Sci & Technol Res Inst, Appl Radiat Res Sch, POB 11365-3486, Tehran, Iran
[3] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran 14176, Iran
[4] Univ Tehran Med Sci, Drug Design & Dev Res Ctr, Tehran 14176, Iran
来源：
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2016年 / 310卷 / 01期
关键词：
Quetiapine; Carbon-14; labeling; Isoclotiapine; Pyridobenzothiazepine; NERVOUS-SYSTEM AGENTS; ATYPICAL ANTIPSYCHOTICS; BIPOLAR DEPRESSION; DOUBLE-BLIND; QUETIAPINE; METABOLITES; CLOZAPINE; PLACEBO;
D O I：
10.1007/s10967-016-4798-1
中图分类号：
O65 [分析化学];
学科分类号：
070302 ; 081704 ;
摘要：
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-C-14]. 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-C-14] by good radiochemical yield. And also isoclotiapine[11-C-14], and 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine[10-C-14], synthesized according to this route.
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收藏
页码：433 / 439
页数：7
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