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-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:US-5113019-A 优先权日:1987-11-27 标 题:Process for phenol alkylthiolation and its application to the synthesis of 4-acyl-2-alkylthiophenols 发明人:VOTTERO CATHERINE; LABAT YVES; POIRIER JEAN-MARIE 权利人:ELF AQUITAINE 摘要:The invention relates to the preparation of alkylthiophenols by reaction of a dialkyl disulphide with a phenol. n In the process according to the invention, the reaction is carried out in the presence of aluminum chloride or of ferric chloride in a solvent of the alkylbenzene type or, soley in the case of methylthiolation, in an excess of dimethyl disulphide. n This process makes it possible, in particular to obtain, with a selectivity and in a yield which are excellent, 2-alkylthiophenols which may then be converted into 4-acyl-2-alkylthiophenols by means of a reaction at a temperature ranging from 40° to 100° C. with a complex BF 3 :2RCOOH where R denotes an alkyl or propenyl radical, in a proportion of 10 to 15 moles of complex per mole of 2-alkylthiophenol.
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.