CAS: 303-49-1; Clomipramine

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CAS号14171-67-6 3-(2-chloro-5,6... | CAS号303-48-0 去甲氯米帕明 盐酸盐 | CAS号14171-67-6 3-(2-chloro-5,6...

2-溴苯胺置于甲醇,Palladium Diacetate,Caesium Carbonate,Magnesium,三苯基膦,Potassium Iodide体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 71.5H,反应生成氯米帕明
参考文献:增强芳基溴化物的反应性和选择性:二苯并[b,F]氮杂环庚烷衍生物的一种补充方法
标题:增强芳基溴化物的反应性和选择性:二苯并[b,F]氮杂环庚烷衍生物的一种补充方法
摘要:二氢二苯并[ B,F ]氮杂和二苯并[ B,F ]氮杂可以通过钯催化从芳基溴化物,邻溴代苯胺和降冰片烯或降冰片二烯有效合成.该协议可以访问二苯并[ B,F]氮杂core核在两个芳环上均包含多个吸电子取代基,并补充了先前报道的方法,在该方法中优先使用富含电子的芳基碘化物.Ki的存在,即使是低于化学计量的量,对于该三组分反应也至关重要.适当添加碘化物阴离子对反应速率和选择性具有显着影响.的三环类抗抑郁药氯米帕明(安那芬尼正式三步合成®)也被描述.
Doi:10.1002/cctc.201800940

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:WO-2015194928-A1
优先权日:2014-06-17
标 题:Method for the isolation and synthesis of 3-(1´, 1´- dimethylallyl)-herniarin, as well as (e)-3-(1´,1´-dimethyl-3´nitro-allyl-herniarin, from casimiroa pubescens, and use thereof as an antidepressant
发明人：MARTÃ?NEZ VÃ?ZQUEZ MARIANO; ESTRADA REYES ROSA; UBALDO SUÃ?REZ DENISSE; DE LA ROSA SIERRA ROBERTO
权利人:UNIV NAC AUTÓNOMA DE MÉXICO
摘要:The invention relates to the compounds 3-(1´,1´ -dimethylallyl)-herniarin (1) y 3- (1,1´-dimethyl-3´ nitro allyl-herniarin] (3) (NHR) derived from coumarin, which have excellent antidepressant activity. The compound 3- (1,1´-dimethyl-3´ nitro allyl-herniarin] (3) (NHR) is synthesised by means of a nitration reaction of the compound 3-(1´,1´-dimethylallyl)-herniarin. The present invention also relates to the method for the isolation and synthesis of the compound 3 -(1´,1´-dimethylallyl)-herniarin.

专利号:US-12234200-B2
优先权日:2019-04-16
标 题:Synthetic methods of preparing esketamine
发明人：CHEN CHENG YI
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.

专利号:US-10905674-B2
优先权日:2017-11-22
标题:Method of increasing melatonin synthesis to treat insomnia, ameliorate sleep disturbance and regulate sleep
发明人：LIN YUNG-HSIANG; YU CHIN-HSIU; SU YU-HUNG; LIN SHAN-YU; CHUNG YU-MING
权利人:TCI CO LTD
摘要:A method for at least one of increasing the synthesis of melatonin and promoting the secretion of melatonin is provided, wherein the method comprises administering to a subject in need an effective amount of a compound of formula (I): n nA method for at least one of treating diseases related to neurometabolic disorder, preventing diseases related to neurometabolic disorder, regulating appetite, regulating mood, regulating vasoconstriction, regulating hemostatic function and regulating immune response is also provided, wherein the method comprises administering to a subject in need an effective amount of a compound of formula (I) as described above.

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.