专利号:US-6846957-B2 优先权日:2002-11-22 标题 :Synthesis of 3-aminomethyl-1-propanol, a fluoxetine precursor 发明人:ZELENIN ALEXANDER 权利人:UNIV TEXAS 摘要:The present invention concerns a method of synthesizing fluoxetine hydrochloride. The method includes the synthesis of 3-methylamino-1-phenyl-1-propanol by reduction of 1-phenyl-3-methylamino-2-propen-1-one with sodium borohydride and acetic acid.
专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-2023399302-A1 优先权日:2020-10-29 标题:Process for the preparation of heteroaryl-substituted sulfur(vi) compounds 发明人:LOPCHUK JUSTIN M; SHULTZ ZACHARY P; SCATTOLIN THOMAS 权利人:H LEE MOFFITT CANCER CT & RES 摘要:The present disclosure provides processes for the synthesis of organic compounds, in particular processes for the synthesis of heteroaryl-substituted sulfur(VI) compounds by nucleophilic aromatic substitution.
专利号:WO-0021917-A1 优先权日:1998-10-13 标题 :Pharmaceutical intermediate for the synthesis of fluoxetine and a process for the preparation thereof 发明人:REITER JOZSEFNE; SIMIG GYULA; MEZEI TIBOR; IMRE JANOS; VERECZKEYNE DONATH GYOERGYI; NAGY KALMAN; NEMETH NORBERT; SZABO TIBOR 权利人:EGYT GYOGYSZERVEGYESZETI GYAR; REITER JOZSEFNE; SIMIG GYULA; MEZEI TIBOR; IMRE JANOS; VERECZKEYNE DONATH GYOERGYI; NAGY KALMAN; NEMETH NORBERT; SZABO TIBOR 摘要:The invention relates to N,N-dimethyl-{3-phenyl-3-[(4-trifluoromethyl)-phenoxy]-propyl-amine}-p-toluenesulfonate of Formula (I) and an improved process for the preparation thereof. The new compound of Formula (I) is a valuable pharmaceutical intermediate useful in the preparation of the antidepressant having the generic name fluoxetine.
专利号:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-5998627-A 优先权日:1997-08-04 标题 :Preparation and uses of hydrocarbylnitrones 发明人:THERIOT KEVIN J 权利人:ALBEMARLE CORP 摘要:Nitrones are produced by reaction of primary amine with aldehyde or ketone, in the presence of a transition metal-containing oxidation catalyst, and a peroxidic compound. The nitrone can then be reacted with a vinylaromatic compound to produce a 2-hydrocarbyl-5-arylisoxazolidine. Both such reactions can be conducted concurrently by including the vinylaromatic compound in the initial reaction mixture. Hydrogenation of the 2-hydrocarbyl-5-arylisoxazolidine, e.g., using hydrogen and a palladium-carbon catalyst, forms an N-hydrocarbyl-3-aryl-3-hydroxypropylamine. Such reactions enable, inter alia, synthesis of the racemic hydrochloride salt of N-methyl-3-phenyl-3-[4-trifluoromethyl)phenoxy]-propylamine, known generically as fluoxetine hydrochloride, a widely used antidepressant.
[参考文献]: Akiko Okamoto, Et Al. Synthesis Of Novel Trifluoromethyl-Bearing Bifunctional Acyl-Acceptant Arenes: 2,2'-Bis(Trifluoromethylated Aryloxy)Biphenyls. J Oleo Sci. 2007;56(9):479-91. [参考文献]: D W Robertson, Et Al. Absolute Configurations And Pharmacological Activities Of The Optical Isomers Of Fluoxetine, A Selective Serotonin-Uptake Inhibitor. J Med Chem. 1988 Jul;31(7):1412-7.
合成参考文献
摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 623. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 96. 摘要:Hari, Y.; Aoyama, T.; Shioiri, T., Science of Synthesis Knowledge Updates, (2010) 4, 45. 摘要:Müller, T., Science of Synthesis Knowledge Updates, (2013) 3, 27. 摘要:Oishi, M.; Takikawa, H., Science of Synthesis Knowledge Updates, (2010) 4, 104.