专利号:US-10562872-B2 优先权日:2016-02-08 标 题 :Synthesis of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine 发明人:DINESS FREDERIK; MELDAL MORTEN; JACOBSEN CHRISTIAN BORCH 权利人:H LUNDBECK AS 摘要:The invention relates to a method for synthesis of 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine in the presence of a strong base.
专利号:US-12180182-B2 优先权日:2021-12-01 标题 :(Di)amination of activated allene compounds, derivatives thereof, and methods for synthesis of the same 发明人:DAI MINGJI 权利人:PURDUE RESEARCH FOUNDATION 摘要:One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.
专利号:US-9493409-B2 优先权日:2013-04-04 标题 :Process for the synthesis of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine 发明人:ZUPANCIC BORUT 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides new intermediate compounds or formulae (III) and (IVa), and salts thereof, and their use in a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine) an experimental drug under development for the treatment of depression and anxiety.
专利号:WO-2014191548-A1 优先权日:2013-05-31 标题:New process for the synthesis of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine 发明人:ZUPANCIC BORUT 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine), an experimental drug under development for the treatment of depression and anxiety, which comprises the reaction of a compound of formula (VII), or salt thereof, (VII) wherein Q represents S, SO or SO 2 and LG represents a leaving group, with a compound of formula (XI), or salt thereof, (XI) wherein Z represents hydrogen or a protecting group. New intermediate compounds are also provided.
专利号:WO-2015107057-A1 优先权日:2014-01-14 标 题:Synthesis of vortioxetine via (2-(piperazine-1 -yl)phenyl)aniline intermediates 发明人:ZUPANCIC BORUT 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides a new synthetic process for the production of 1-(2-((2,4- dimethylphenyl)thio)phenyl)piperazine (vortioxetine), a drug for the treatment of depression and anxiety, which is conducted via (2-(piperazine-1-yl)phenyl)aniline intermediates.
专利号:WO-2015079018-A1 优先权日:2013-11-29 标题:Synthesis of vortioxetine via (2-(piperazine-1 -yl)phenvl)lithium intermediates 发明人:ZUPANCIC BORUT; STERK DAMJAN; MARAS NENAD 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides a new synthetic process for the production of 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine (vortioxetine), a drug for the treatment of depression and anxiety, which is conducted via (2-(piperazine-1-yl)phenyl)lithium intermediates.
1: Berardelli I, Rogante E, Formica F, Iannazzo R, Mammoliti AV, Riccioni R, Veizi S, McIntyre RS, Pompili M. The efficacy of vortioxetine in the acute treatment of major depressive disorder: A systematic review and meta-analysis. J Psychopharmacol. 2025 Feb 1:2698811241309612. doi: 10.1177/02698811241309612. Epub ahead of print. 26(1):26-38. doi: 10.1631/jzus.B2400470. 4: Erkilinc G, Ozdamar G, Ozmen O, Yüceer RO. Effect of vortioxetine and fluoxetine on immunohistochemical expression of Caspase-8, RANKL, and IL-6 in testicular tissue in an experimental depression model. Biotech Histochem. 2025 Jan
合成参考文献
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