CAS: 139079-39-3; 6-[4-[2-(2-Hydroxyethoxy)Ethyl]Piperazin-1-Yl]Benzo[b][1,4]Benzothiazepin-2-Ol

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7-Benzyloxy Quetiapine 329217-58-5
7-苄氧基-11-氯二苯并[b,F[[1,4]硫氮杂卓 7-Benzyloxy-11-Chlorodibenzo[b,F][1,4]Thiazepine 1076198-96-3

📜1-[2-(2-羟基乙氧基)乙基]哌嗪置于氢氧化钾,氢溴酸体系中,用 甲醇,Xylene 用作溶剂,化学反应 23.0H,反应生成7-羟基 喹硫平杂质
参考文献:Behavioral Approach To Nondyskinetic Dopamine Antagonists: Identification Of Seroquel
标题:Behavioral Approach To Nondyskinetic Dopamine Antagonists: Identification Of Seroquel
摘要:A Great Need Exists For Antipsychotic Drugs Which Will Not Induce Extrapyramidal Symptoms (Eps) And Tardive Dyskinesias (Tds). These Side Effects Are Deemed To Be A Consequence Of Nonselective Blockade Of Nigrostriatal And Mesolimbic Dopamine D2 Receptors. Nondyskinetic Clozapine (1) Is A Low-Potency D2 Dopamine Receptor Antagonist Which Appears To Act Selectively In The Mesolimbic Area. In This Work Dopamine Antagonism Was Assessed In Two Mouse Behavioral Assays: Antagonism Of Apomorphine-Induced Climbing And Antagonism Of Apomorphine-Induced Disruption Of Swimming. The Potential For The Liability Of Dyskinesias Was Determined In Haloperidol-Sensitized Cebus Monkeys. Initial Examination Of A Few Close Cogeners Of 1 Enhanced Confidence In The Cebus Model As A Predictor Of Dyskinetic Potential. Considering Dibenzazepines,2 Was Not Dyskinetic Whereas 2A Was Dyskinetic. Among Dibenzodiazepines,1 Did Not Induce Dyskinesias Where As Its N-2-(2-Hydroxyethoxy)Ethyl Analogue 3 Was Dyskinetic. The Emergence Of Such Distinctions Presented An Opportunity. Thus,Aromatic And N-Substituted Analogues Of 6-(Piperazin-1-yl)-11H-Dibenz[b,E]Azepines And 11-(Piperazin-1-yl)Dibenzo[b,F][1,4]Thiazepines And-Oxazepines Were Prepared And Evaluated. 11-(4-[2-(2-Hydroxyethoxy)Ethyl]Piperazin-1-yl)Dibenzo[b,F][1,4]Thiazepine (23) Was Found To Be An Apomorphine Antagonist Comparable To Clozapine. It Was Essentially Nondyskinetic In The Cebus Model. With 23 As A Platform,A Number Of N-Substituted Analogues Were Found To Be Good Apomorphine Antagonists But All Were Dyskinetic.
Doi:10.1021/jm000242+

专利信息

专利号:US-9304126-B2
优先权日:2012-08-21
标题:Haptens of quetiapine
发明人：DONAHUE MATTHEW GARRETT; GONG YONG; SALTER RHYS; HRYHORENKO ERIC; DECORY THOMAS R; REMMERIE BART; SANKARAN BANUMATHI
权利人:JANSSEN PHARMACEUTICA NV; ORTHO CLINICAL DIAGNOSTICS INC
摘要:The invention relates to compounds of Formula I, wherein R 1 , R 2 , and R 3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from quetiapine. The invention also relates to conjugates of a quetiapine hapten and a protein.