CAS: 98769-81-4; Reboxetine

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    morpholin-3-one(2RS,3RS)-6-α-(2-ethoxyphenoxy)benzylmorpholin-3-one 2-Ethoxyphenol benzaldehyde trans-2,3-epoxy-3-phenylpropan-1-olReboxetine mesylate (S,S)-reboxetine (2R,3R)-reboxetine morpholine methanesulfonate(2RS,3SR)-2-α-(2-ethoxyphenoxy)benzylmorpholine methanesulfonate

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      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-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.

      专利号:US-10266503-B1
      优先权日:2016-05-24
      标 题 :Sulfoxide ligand metal catalyzed oxidation of olefins
      发明人:WHITE M CHRISTINA; AMMANN STEPHEN E; LIU WEI; MA RULIN
      权利人:UNIV ILLINOIS
      摘要:The enantioselective synthesis of isochroman motifs has been accomplished via Pd(II)-catalyzed allylic C—H oxidation from terminal olefin precursors. Critical to the success of this goal was the development and utilization of a novel chiral aryl sulfoxide-oxazoline (ArSOX) ligand. The allylic C—H oxidation reaction proceeds with the broadest scope and highest levels asymmetric induction reported to date (avg. 92% ee, 13 examples ≥90% ee). Additionally, C(sp 3 )-N fragment coupling reaction between abundant terminal olefins and N-triflyl protected aliphatic and aromatic amines via Pd(II)/sulfoxide (SOX) catalyzed intermolecular allylic C—H amination is disclosed. A range of 52 allylic amines are furnished in good yields (avg. 76%) and excellent regio- and stereoselectivity (avg. >20:1 linear:branched, >20:1 E:Z). For the first time, a variety of singly activated aromatic and aliphatic nitrogen nucleophiles, including ones with stereochemical elements, can be used in fragment coupling stiochiometries for intermolecular C—H amination reactions.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
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      合成参考文献


      摘要:Yu, Z. W.; Yeung, Y.-Y., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 2, 306.
      参考文献:10.1016/s0368-2315(06)76416-x
      摘要:Debodinance P, Cosson M, Collinet P, Boukerrou M, Lucot JP, Madi N. [Synthetic meshes for transvaginal surgical cure of genital prolapse: evaluation in 2005]. J Gynecol Obstet Biol Reprod (Paris). 2006 Sep;35(5 Pt 1):429–54. doi: 10.1016/s0368-2315(06)76416-x.
      参考文献:10.1016/j.bmcl.2008.05.077
      摘要:Zhang M, Jovic F, Vickers T, Dyck B, Tamiya J, Grey J, Tran JA, Fleck BA, Pick R, Foster AC, Chen C. Studies on the structure–activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorganic & Medicinal Chemistry Letters. 2008 Jul;18(13):3682–6. doi: 10.1016/j.bmcl.2008.05.077.
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