蒽酮置于ammonium Hydroxide,Lithium Aluminium Tetrahydride,草酰氯,锌体系中,用 乙醚,N,N-二甲基甲酰胺 用作溶剂,化学反应生成马普替林 参考文献:[1-氨基烷基-二苯并(b,E)双环(2,2,2)辛二烯的合成和性质]. 标题:[1-氨基烷基-二苯并(b,E)双环(2,2,2)辛二烯的合成和性质]. 摘要:Abstractthe Syntheses Of Dibenzo [b,E] Bicyclo [2.2.2] octadienes Substituted At The Bridgehead By Aminomethyl,Aminoethyl Or Aminopropyl Groups Are Described. The Influence Of This Substitution On The Fragmentation Upon Electron Impact And On The NMR Spectra Of The New Compounds Is Discussed. Doi:10.1002/hlca.19690520602
专利信息
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
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: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-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-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.
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合成参考文献
参考文献:10.1007/s00221-005-0228-2 摘要:Tan CH, He X, Yang J, Ong WY. Changes in AMPA subunit expression in the mouse brain after chronic treatment with the antidepressant maprotiline: a link between noradrenergic and glutamatergic function Exp Brain Res. 2006 Apr;170(4):448–56. doi: 10.1007/s00221-005-0228-2. 参考文献:10.1055/s-0031-1279729 摘要:Andjelkovic M, Jovanovic DB, Zdravkovic N, Jankovic SM. Gallbladder emptying in patients with major depression: a case series. Pharmacopsychiatry. 2011 Jul;44(5):165–8. doi: 10.1055/s-0031-1279729. 参考文献:10.4103/0019-5545.82567 摘要:Ramachandraih CT, Subramanyam N, Bar KJ, Baker G, Yeragani VK. Antidepressants: From MAOIs to SSRIs and more. Indian J Psychiatry. 2011 Apr;53(2):180–2. 参考文献:10.1007/s10549-005-9056-0 摘要:Chien C, Li CI, Heckbert SR, Malone KE, Boudreau DM, Daling JR. Antidepressant use and breast cancer risk. Breast Cancer Research and Treatment. 2005 Dec 02;95(2):131–40. doi: 10.1007/s10549-005-9056-0. 参考文献:10.1007/s00535-005-1687-8 摘要:Hojo M, Miwa H, Yokoyama T, Ohkusa T, Nagahara A, Kawabe M, Asaoka D, Izumi Y, Sato N. Treatment of functional dyspepsia with antianxiety or antidepressive agents: systematic review. J Gastroenterol. 2005 Nov;40(11):1036–42. doi: 10.1007/s00535-005-1687-8.