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.

引用

页码：433 / 439

页数：7

共 50 条

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