CAS: 635705-72-5; (S)-4-Amino-2-(1-(3-Ethoxy-4-Methoxyphenyl)-2-(Methylsulfonyl)Ethyl)Isoindoline-1,3-Dione

该化合物是Aprimilast(一种磷柴油酶4(PDE4)抑制剂)的衍生物,主要用于制药研究,作为合成亚丙米拉斯和相关化合物的参考标准或中间体;该化合物保留亚丙酰甲状腺的核心结构,但缺乏可能影响其药用动力学和药用动力学特性的乙酰基.

结构式图片

上下游产品

2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulfonyl)eth-2-ylamine (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine-(S)-2-acetamido-4-methylpentanoate 3-aminophthalic acid (S)-2-[1 (3-ethoxy-4-methoxyphenyl)]-1-methanesulfonyl-2-ethylamine(1S)-2-benzyloxy-N-{2-[1-(3-ethoxy-4-methoxy-phenyl)-2-methanesulfonyl-ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}-acetamide (S)-4-Amino-2-[1-(3,4-dihydroxy-phenyl)-2-methanesulfonyl-ethyl]-isoindole-1,3-dione (S)-N-{2-[1-(3-ethoxy-4-hydroxy-phenyl)-2-methanesulfonyl-ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}-2-hydroxy-acetamide (S)-N-{2-[1-(3,4-dihydroxy-phenyl)-2-methanesulfonyl-ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}-2-hydroxy-acetamide

合成工艺路线路线简述

    📜阿普斯特置于盐酸体系中,用 甲醇 作为反应溶剂,以8 G的收率获得产物阿普斯特降解杂质
    参考文献: Process For Preparation Of Apremilast[fr] Procédé De Préparation D'Aprémilast
    标题: Process For Preparation Of Apremilast[fr] Procédé De Préparation D'Aprémilast
    摘要:本发明涉及一种制备阿普利莫司特的方法.本发明涉及阿普利莫司特的对二甲苯溶剂结晶体以及其制备方法.

    海关参考信息

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    参考标题:Asymmetric Synthesis Of β-Aryl β-Imido Sulfones Using Rhodium Catalysts With Chiral Diene Ligands: Synthesis Of Apremilast
    作者:Jin-Fong Syu,Balraj Gopula,Jia-Hong Jian,Wei-Sian Li,Ting-Shen Kuo,Ping-Yu Wu,Julian P. Henschke,Meng-Chi Hsieh,Ming-Kang Tsai,Hsyueh-Liang Wu |发布日期:2019.6.21
    摘要:A Chiral Rhodium(I)-Diene Catalyst Enabled The One-Step Synthesis Of β-Aryl β-Imido Sulfones Under Mild Reaction Conditions. By Selection Of The Chiral Diene Ligand L1A Or L2, Each Enantiomer Of The Chiral β-Aryl β-Imido Sulfone Target Can Be Accessed With High Stereoselectivity. Demonstration Of The Scope Of The Reaction, Which Includes The Synthesis Of An N-Protected Chiral β-Amino β-Phenyl Sulfone

    合成参考文献


    摘要:S113 | SWISSPHARMA24 | 2024 Swiss Pharmaceutical List with Metabolites | DOI:10.5281/zenodo.10501043
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