邻二氯苯置于n-溴代丁二酰亚胺(Nbs),N-碘代丁二酰亚胺,Magnesium,Lithium Chloride体系中,用 溶剂黄146 作为反应溶剂,化学反应 41.0H,反应生成 邻碘溴苯 参考文献:Copper-Free Double Silylation Of 1,2-Dibromobenzenes Using A Mg/licl/dmi System 标题:Copper-Free Double Silylation Of 1,2-Dibromobenzenes Using A Mg/licl/dmi System 摘要:1,2-二溴苯与氯三甲基硅烷在dmi中在温和条件下,在mg和licl存在下高效进行反应,产率非常好至高.1,2-二溴苯与氯二甲基硅烷在相同条件下反应,得到相应的1,2-二(二甲基硅基)苯,产率高.对1,2-二(三甲基硅基)苯进行了功能团转化,以展示其合成效用. DOI:10.1055/s-0036-1588726
专利信息
专利号:EP-2103609-A1 优先权日:2008-03-20 标 题:Catalyzed carbonylation in the synthesis of angiotensin ii antagonists 权利人:LEK PHARMACEUTICALS 摘要:One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
专利号:US-8445693-B2 优先权日:2008-03-20 标 题 :Catalyzed carbonylation in the synthesis of angiotensin II antagonists 发明人:CASAR ZDENKO; COPAR ANTON; CLUZEAU JEROME; PREMRL ANDREJ 权利人:CASAR ZDENKO; COPAR ANTON; CLUZEAU JEROME; PREMRL ANDREJ; LEK PHARMACEUTICALS 摘要:One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3′-(2′-halo-biphenyl-4-ylmethyl)-1,7′-dimethyl-2′-propyl-1H,3′H-[2,5′]bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
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:WO-2018217538-A1 优先权日:2017-05-23 标题 :Synthesis of substituted acridines 发明人:FORT ERIC H; JAYE JOSEPH A; MCCORMICK GRANT M; BERGER KRISTEN E 权利人:UNIV OF ST THOMAS 摘要:Disclosed is a method of making substituted acridines. The method includes the step of reacting a bis(halophenyl) amine with an alkyne for a time and at a temperature to yield a substituted acridine.
专利号:US-10865163-B2 优先权日:2017-12-20 标题:Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds 发明人:YOUNG MICHAEL C; KAPOOR MOHIT 权利人:UNIV TOLEDO 摘要:Methods of synthesizing compounds using CO 2 as a directing group for C—H functionalization, and compounds made thereby, are described.
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.
[参考文献]: Lei Liu, Et Al. Stability-Indicating Reversed-Phase Hplc Method Development And Characterization Of Impurities In Vortioxetine Utilizing Lc-Ms, Ir And Nmr. J Pharm Biomed Anal. 2016 Jan 5:117:325-32.
合成参考文献
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