CAS: 175591-09-0; Tapentadol Hydrochloride

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tapentadol (-)-(2S,3S)-1-dimethylamino-3-(3-methoxy-phenyl)-2-methyl-pentan-3-ol hydr°Chloride 3'-nitropropiophenone 3-dimethylamino-2-methyl-1-(m-nitrophenyl)-1-propanonetapentadol

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    📜他喷他多置于盐酸体系中,用 二氯甲烷,异丙醚 用作溶剂,化学反应 0.5H,反应生成盐酸他喷他多
    参考文献: Process For Preparing L-Phenyl-3-Dimethylaminopropane Derivative[fr] Procédé De Préparation De Dérivés De L-Phényl-3-Diméthylaminopropane
    标题: Process For Preparing L-Phenyl-3-Dimethylaminopropane Derivative[fr] Procédé De Préparation De Dérivés De L-Phényl-3-Diméthylaminopropane
    摘要:提供了一种制备l-苯基-3-二甲氨基丙烷衍生物的过程,其化学式为i,并通过新颖的中间体制备其药用可接受的盐.

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    专利信息


    专利号:US-2013296608-A1
    优先权日:2011-01-27
    标 题 :Novel stereospecific synthesis of (-) (2s, 3s)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol
    发明人:MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU
    权利人:MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU; SYMED LABS LTD
    摘要:The present invention relates to a novel stereospecific synthesis of (−)(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol.

    专利号:US-2013150622-A1
    优先权日:2011-12-12
    标题:Stereoselective synthesis of tapentadol and its salts
    发明人:FANDRICK DANIEL ROBERT; RODRIGUEZ SONIA; YANG BING-SHIOU
    权利人:BOEHRINGER INGELHEIM INT; BOEHRINGER INGELHEIM INT
    摘要:A process for the synthesis of a salt of tapentadol.

    专利号:US-8729308-B2
    优先权日:2009-12-01
    标 题:Process for the preparation of tapentadol and intermediates thereof
    发明人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO
    权利人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; EUTICALS SPA
    摘要:The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below n nusing the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative.n n The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

    专利号:WO-2012089181-A1
    优先权日:2010-12-30
    标题 :O-substituted (2r,3r)-3-(3-hydroxyphenyl)-2-methyl-4-pentenoic acids and a method of obtaining the same
    发明人:VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF
    权利人:ZENTIVA KS; VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF
    摘要:The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.

    专利号:US-2013046012-A1
    优先权日:2010-04-28
    标题 :New compounds, synthesis and use thereof in the treatment of pain
    发明人:DEL CASTILLO NIETO JUAN CARLOS; MOURELLE MANCINI MARISABEL; PUBILL COY FRANCISCO; REPOLLES MOLINER JOSE
    权利人:LACER SA; DEL CASTILLO NIETO JUAN CARLOS; MOURELLE MANCINI MARISABEL; PUBILL COY FRANCISCO; REPOLLES MOLINER JOSE
    摘要:The present invention relates to compounds of formula (I), or pharmaceutically acceptable, stereoisomers, salts or solvates thereof n n n n n n n n n n to methods for their synthesis, and use in the treatment of pain.

    专利号:EP-4630405-A1
    优先权日:2022-12-06
    标题 :Process for the synthesis of substituted tetrahydrofuran modulators of sodium channels

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    合成参考文献


    摘要:https://pubs.acs.org/doi/abs/10.1021/acs.analchem.7b01709
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