CAS: 51012-32-9; Tiapride

结构式图片

上下游产品

1,4-dioxane 2-methoxy-5-methylsulphonylbenzoic acid N,N-diethylethylenediamine

合成工艺路线路线简述

  • 合成目标产物 Tiapride 主要起始原料 2-Methoxy-5-(Methylsulfonyl)Benzoic Acid
  • (文献来源)合成步骤主要原料 2-Methoxy-5-(Methylsulfonyl)Benzoic Acid
硫比利置于三乙胺体系中,用 乙腈 作为反应溶剂,化学反应 5.0H,反应生成 硫必利
参考文献:通过活性α-酰基烯醇酯中间体直接酰胺化羧酸
标题:通过活性α-酰基烯醇酯中间体直接酰胺化羧酸
摘要:描述了使用壬酸酯作为新型偶联剂来开发用于羧酸的直接酰胺化的高效且简单的方案.通过在温和的反应条件下原位形成α-酰基烯醇酯中间体,可将转化率以非常好至极好的收率进行.已经证明了这种有用的方法可用于多种底物,以提供对结构多样的酰胺的简洁访问,包括格列本脲,替阿必利盐酸盐和那格列奈的关键中间体,并且可以以摩尔规模进行.
DOI:10.1021/acs.Joc.8B00819

海关参考信息

专利信息


专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人:BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-2012282255-A1
优先权日:2011-04-07
标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
发明人:PLUCINSKI GREG
权利人:PLUCINSKI GREG
摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

专利号:US-7300639-B2
优先权日:2002-12-03
标 题:Process for removing metals from liquids
发明人:LIU WANSHENG
权利人:BRISTOL MYERS SQUIBB CO
摘要:A process is provided for removing one or more metals from liquids. Also provided is a process for the synthesis of aP2 inhibiting compounds having the formula (I) n nwherein R 1 , R 2 , R 3 , R 4 , HET, and X-Z are as described herein, which process comprising the step of removing one or more metals from a solution of the compound of formula I or an intermediate or precursor thereof. The processes for removing metal comprise the step of contacting the liquid with a solid extractant comprising a metal-binding functionality.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
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合成参考文献


参考文献:10.3389/fnsys.2011.00055
摘要:West AR, Tseng KY. Nitric Oxide-Soluble Guanylyl Cyclase-Cyclic GMP Signaling in the Striatum: New Targets for the Treatment of Parkinson's Disease Front Syst Neurosci. 2011;5():55.
参考文献:10.1097/adm.0b013e3181ec5f81
摘要:Müller CA, Schäfer M, Banas R, Heimann HM, Volkmar K, Förg A, Heinz A, Hein J. A combination of levetiracetam and tiapride for outpatient alcohol detoxification: a case series. J Addict Med. 2011 Jun;5(2):153–6. doi: 10.1097/adm.0b013e3181ec5f81.
参考文献:10.4137/ccrep.s5812
摘要:Hiroi N, Yoshihara A, Sue M, Yoshino G, Higa M. Central adrenal insufficiency and diabetes insipidus misdiagnosed as severe depression. Clin Med Insights Case Rep. 2010;3():55–8.
参考文献:10.3389/fnsys.2011.00049
摘要:Collins-Praino LE, Paul NE, Rychalsky KL, Hinman JR, Chrobak JJ, Senatus PB, Salamone JD. Pharmacological and physiological characterization of the tremulous jaw movement model of parkinsonian tremor: potential insights into the pathophysiology of tremor. Front Syst Neurosci. 2011;5():49.
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