CAS: 6104-71-8; N-Desmethylclozapine
- 英文名称N-Desmethylclozapine
- 中文名称8-氯-11-(1-哌嗪基)-5H-二苯并[B,E] [1,4]吡喃
- IUPAC名称8-chloro-11-(piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine
- 其它别名Demethylclozapine; Desmethylclozapine; N-Demethylclozapine; N-Desmethylclozapine; Norclozapine
- CAS编号6104-71-8
- MFCD编号:MFCD00210189
- EINECS号:636-421-7
- FDA UNII编号:1I9001LWY8
- 分子式:C17H17ClN4分子量:312.8
- 产品CID: 1591762
- 产品分类分析化学 → 标准品 → 标准物质
物理性质
MSDS等安全信息
- GHS象形图
- GHS符号GHS07;
注释: Exclamation mark - 危险类别急性毒性 类别4(吸入)
急性毒性 类别4(经口)
特定目标器官毒性 - 单次接触 类别3
皮肤腐蚀/刺激 类别2
严重眼刺激 类别2 - 警示词Warning(警告)
- 危险描述H332 |吸入有害.
H302 |吞咽有害.
H335 |可能引起呼吸道刺激.
H315 |造成皮肤刺激.
H319 |造成严重眼刺激. - 防范说明P261-P264-P301+P312-P302+P352-P304+P340+P312-P305+P351+P338
- 危险等级6.1(b)
- UN编号3249
- 危险品标志Xn,T,F
- 包装等级III
- 安全声明22-36-45-36/37-16-7
- 危险类别码20/22-36/37/38-39/23/24/25-23/24/25-11
- WGK Germany3
欧盟法规
ECHA物质C&L通报上下游产品
CAS号110-85-0 哌嗪 | CAS号50892-62-1 8-氯-5,10-二氢-11H... | CAS号5786-21-0 氯氮平 | CAS号41513-04-6 1-溴-4-氯-2-硝基苯 | CAS号67990-66-3 N-(2-氨基-4-氯苯基)邻氨基苯甲酸 | CAS号60091-87-4 2-(4-氯-2-硝基苯基)氨基苯甲酸 | CAS号118-92-3 邻氨基苯甲酸合成工艺路线路线简述
- 合成目标产物 N-Desmethylclozapine 主要起始原料 Piperazine And 8-Chloro-5,10-Dihydrodibenzo[b,E][1,4]Diazepin-11-One
- (文献来源)合成步骤主要原料 Piperazine 和 8-Chloro-5,10-Dihydrodibenzo[b,E][1,4]Diazepin-11-One
📜2-溴-5-氯硝基苯置于sodium Dithionite,四氯化钛,铜,Potassium Carbonate体系中,用 1,4-二氧六环,Ammonium Hydroxide,Xylene 作为反应溶剂,化学反应 124.0H,反应生成 8-氯-11-(1-哌嗪基)-5H-二苯并[b,E] [1,4]吡喃
参考文献:氯氮平 4´-芳甲基类似物的合成及初步药理评价.一,芳香族取代基的影响
标题:氯氮平 4´-芳甲基类似物的合成及初步药理评价.一,芳香族取代基的影响
摘要:作为开发具有混合多巴胺 D4 和 5-Ht2A 拮抗剂活性且具有治疗精神分裂症潜力的化合物的研究计划的一部分,我们报告了基于非典型抗精神病药物氯氮平 (2) 的结构修饰的化合物家族.描述了一系列 4'-芳甲基氯氮平类似物的化学合成,结构表征和药理学评价.提供了初步的受体结合数据,主要检查取代基对引入的芳甲基的电子和位置影响,其次是芳环的性质.
DOI:10.1071/ch02093
海关参考信息
- 2902300000-甲苯
2903919090-氯苯
2921211000-乙二胺
2921440000-二苯胺 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2006205714-A1
优先权日:2004-04-01
标 题 :Method of synthesis and isolation of solid N-desmethylclozapine and crystalline forms thereof
发明人：TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG
权利人:TOLF BO-RAGNAR; THYGESEN MIKKEL B; BLATTER FRITZ; BERGHAUSEN JORG
摘要:Disclosed herein are crystalline Forms A, B, C, D, and E of N-desmethylclozapine, methods of preparing the same, pharmaceutical compositions comprising the same, and methods of therapeutic treatment involving N-desmethylclozapine polymorphic forms.
专利号:WO-2009035652-A1
优先权日:2007-09-13
标 题 :Synthesis of deuterated catechols and benzo[d][1,3] dioxoles and derivatives thereof
专利号:WO-2011011384-A9
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2014336387-A1
优先权日:2007-09-13
标题:Synthesis of deuterated catechols and benzo[d][1,3]dioxoles and derivatives thereof
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Anderson SG, Livingston M, Couchman L, Smith DJ, Connolly M, Miller J, Flanagan RJ, Heald AH. Sex differences in plasma clozapine and norclozapine concentrations in clinical practice and in relation to body mass index and plasma glucose concentrations: a retrospective survey. Ann Gen Psychiatry. 2015 Nov 14;14:39. doi: 10.1186/s12991-015-0075-x.
2: Couchman L, Subramaniam K, Fisher DS, Belsey SL, Handley SA, Flanagan RJ. Automated Analysis of Clozapine and Norclozapine in Human Plasma Using Novel Extraction Plate Technology and Flow-Injection Tandem Mass Spectrometry. Ther Drug Monit. 2016 Feb;38(1):42-9. doi: 10.1097/FTD.0000000000000231. doi: 10.1016/j.clinbiochem.2014.09.021. doi: 10.1186/1479-5876-12-203.
5: Couchman L, Belsey SL, Handley SA, Flanagan RJ. A novel approach to quantitative LC-MS/MS: therapeutic drug monitoring of clozapine and norclozapine using isotopic internal calibration. Anal Bioanal Chem. 2013 Nov;405(29):9455-66. doi: 10.1007/s00216-013-7361-8. doi: 10.1016/j.mehy.2012.12.024. doi: 10.1038/aps.2012.71.
合成参考文献
参考文献:10.1111/j.1600-0722.2009.00696.x
摘要:Ekström J, Godoy T, Riva A. N‐Desmethylclozapine exerts dual and opposite effects on salivary secretion in the rat. European J Oral Sciences. 2010 Feb;118(1):1–8. doi: 10.1111/j.1600-0722.2009.00696.x.
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