CAS: 202534-94-9; Ethyl 4-(4-Fluorophenyl)-1-Methyl-2,6-Dioxopiperidine-3-Carboxylate

该化合物是一种氟化管里衍生物,可能用于制药和有机合成,其结构具有4-氟联苯替代物和1-甲基-2,6-二氧基丙基丁基核心,有助于其作为药用化学中间体的再活性.乙基碳本体组会提高溶解性并促进进一步的功能化.该化合物可作为生物活性分子合成的前体,特别是针对...

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    CAS号71510-95-7 N-甲基丙二酸单乙酯单酰胺 | CAS号459-57-4 对氟苯甲醛 | CAS号391937-08-9 trans-3-ethoxyc... | CAS号74-88-4 碘甲烷 | CAS号318279-38-8 反式-4-(4-氟苯基)-3-...

    合成工艺路线路线简述

    • 合成目标产物 Ethyl 4-(4-Fluorophenyl)-1-Methyl-2,6-Dioxopiperidine-3-Carboxylate 主要起始原料 Ethyl-N-Methyl Malonamide And 4-Fluorobenzaldehyde And Acetic Acid
    • (文献来源)合成步骤主要原料 Ethyl-N-Methyl Malonamide 和 4-Fluorobenzaldehyde 和 Acetic Acid
    📜N-甲基丙二酸单乙酯单酰胺,对氟苯甲醛置于sodium Methylate,溶剂黄146体系中,用 水,乙酸乙酯 用作溶剂,化学反应生成4-(4-氟苯基)-1-甲基-2,6-二氧代哌啶-3-羧酸乙酯
    参考文献:Process For Preparing Aryl-Piperidine Carbinols And Novel Intermediates
    标题:Process For Preparing Aryl-Piperidine Carbinols And Novel Intermediates
    摘要:公开了一种制备化合物的过程,其化学式为(I):其中ar是芳基或取代芳基,R.Sup.3是氢,烷基或芳基烷基,该过程包括还原化合物的过程的化学式(II):其中ar和r.Sup.3如与式(I)相关定义,R.Sup.4是烷基.化合物的化学式(I)可用作化学中间体.

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    专利信息


    专利号:WO-2015071831-A1
    优先权日:2013-11-18
    标 题 :An improved process for minimising the formation of dehalogenated byproducts
    发明人:KADAM SHASHIKANT; ARADDY RAJSHEKAR; KONDRAGUNTA VENKATESWARA RAO; HULAVALE YOGESH; SOMISETTI NARENDER RAO; CHENNAMSETTY SUNEEL MANOHAR BABU; HARIHARAN SIVARAMAKRISHNAN
    权利人:PIRAMAL ENTPR LTD
    摘要:The present invention provides an improved process for preparation of organic compounds represented by Formula-Z; wherein effectively minimising the formation of dehalogenated by-products is achieved. In the process, the reduction is carried out using suitable reducing agent; more preferably Lithium Aluminium Hydride (LAH) in a solvent system, wherein at least one of the solvent is selected from halogenated solvents, which acts as co-solvent. The process of the present invention is useful for minimising of the formation of dehalogenated by-products during synthesis of various active pharmaceutical ingredients such as Paroxetine Hydrochloride, Cinacalcet, Eletriptan and Asenapine.

    专利号:US-2001053862-A1
    优先权日:1998-12-22
    标 题:Process for preparing arylpiperidine carbinol intermediates and derivatives
    发明人:RONSEN BRUCE; UPADHYAYA SUBHASH P
    摘要:A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed. A preferred process embodiment provides the synthesis of intermediate compounds of structural formula (I) and structural formula (II): n n n where X is halo, C 1 -C 10 alkoxy, C 1 -C 10 haloalkyl, or hydroxy; R 2 and R 3 are each C 1 -C 4 alkyl, and R 2 and R 3 are the same. The compound of structural formula (I) is made by condensing a corresponding cinnamonitrile with a corresponding diester malonate. The compound of structural formula (II) in the (±)-trans configuration is obtained by hydrogenating the compound of structural formula (I). The compounds of structural formula (I) and structural formula (II) are useful chemical intermediates for synthesizing 4-arylpiperidine-3-carbinols and their derivatives in (−)-trans configuration.

    专利号:WO-2009005647-A2
    优先权日:2007-06-27
    标 题 :Compounds and process to prepare chiral intermediates for synthesis of paroxetine

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    主要参考文献

    参考标题:Catalytic Michael/ring-Closure Reaction Of α,β-Unsaturated Pyrazoleamides With Amidomalonates: Asymmetric Synthesis Of (−)-Paroxetine
    作者:Yu Zhang,Yuting Liao,Xiaohua Liu,Qian Yao,Yuhang Zhou,Lili Lin,Xiaoming Feng |发布日期:2016.10.10
    摘要:A Highly Enantioselective Tandem Michael/ring‐closure Reaction Of α,β‐unsaturated Pyrazoleamides And Amidomalonates Has Been Accomplished In The Presence Of A Chiral N,N′‐dioxide-Yb(Otf)3 Complex (Tf: Trifluoromethanesulfonyl) To Give Various Substituted Chiral Glutarimides With High Yields And Diastereo‐ And Enantioselectivities. Moreover, This Methodology Could Be Used For Gram‐scale Manipulation
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