CAS: 884494-44-4; (2-Chloro-4-Iodopyridin-3-yl)Methanol

该化合物是一种卤化的丙烯衍生物,在三处有一个氢氧化甲基功能组,使其成为有机合成的多用途中间体,其独特的替代模式--二处的氯和四处的碘,为交叉反应(如铃木或松冈竹木木合金)选择性反应反应反应而提供替代,如铃木或松冈竹木,从而能够构建复杂的环流框架.氢氧化甲基组通过充当衍生或聚合处理器,进一步提高效用.这一化合物在制药和农用化学研究中特别有用,其结构特征有利于目标生物活性分子的开发.在标准条件下的高纯度和稳定性确保合成应用的可靠性能.

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2-Chloro-4-iodo-3-pyridinecarboxaldehyde

合成工艺路线路线简述

    📜2-氯-4-碘吡啶-3-甲醛置于sodium Tetrahydroborate体系中,用 甲醇 作为反应溶剂,以89 %的收率获得产物2-氯-4-碘吡啶-3-甲醇
    参考文献: Hydroxyamide Derivative And Use Thereof[fr] Dérivé D'Hydroxyamide Et Son Utilisation[zh] 一种羟基酰胺类衍生物及其应用
    标题: Hydroxyamide Derivative And Use Thereof[fr] Dérivé D'Hydroxyamide Et Son Utilisation[zh] 一种羟基酰胺类衍生物及其应用
    摘要:本申请提供一种式(I)所示的羟基酰胺类衍生物,其互变异构体,立体异构体,溶剂化物,代谢产物,同位素标记的化合物,药学上可接受盐或共晶;本申请提供的化合物对hdac及lsd1均有抑制作用,可用于治疗由lsd1和/或hdac介导的疾病.

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    专利信息


    专利号:WO-2015131100-A1
    优先权日:2014-02-28
    标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
    发明人:YU JIN-QUAN
    权利人:SCRIPPS RESEARCH INST
    摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

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    📌 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: Ligand-Controlled C(Sp3)-H Arylation And Olefination In Synthesis Of Unnatural Chiral Alpha Amino Acids Arylation Commandée Par Ligand De C(Sp3)-H Et Oléfination Utilisables Dans Le Cadre De La Synthèse D'Acides Alpha-Aminés Chiraux Non Naturels
    摘要:The Use Of Ligands To Tune The Reactivity And Selectivity Of Transition Metal-Catalysts For C(-Sp3)-H Bond Functionalization Is A Central Challenge In Synthetic Organic Chemistry. Herein, We Report A Rare Example Of Catalyst-Controlled C(Sp3)-H Arylation Using Pyridine And Quinoline Derivatives: The Former Promotes Exclusive Monoarylation, Whereas The Latter Activates The Catalyst Further To Achieve Diarylation. Successive Application Of These Ligands Enables The Sequential Diarylation Of A Methyl Group In An Alanine Derivative With Two Different Aryl Iodides, Affording A Wide Range Of β-Ar-P-Ar ' -Cc-Amino Acids With Excellent Levels Of Diastereoselectivity (D.R. > 20:1). Both Configurations Of The β-Chiral Center Can Be Accessed By Choosing The Order In Which The Aryl Groups Are Installed. The Use Of A Quinoline Derivative As A Ligand Also Enables C(Sp3)-H Olefination Of A Protected Alanine.
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