CAS: 1334674-88-2; (2-Bromo-5H-Pyrrolo[2,3-B]Pyrazin-7-yl)Methanol

该化合物是一种环溴溴化热聚氨酯衍生物,在7号位置有一个氢氧化甲基功能组,该化合物是有机合成的多种中间体,特别是在研制药剂和生物活性分子方面.2号位置的溴替代物可增强对交错反应的再活动,如Suzuki或Buchwald-Hartwig, 能够有效地衍生.氢氧甲基化合物通过氧化,酯化或醚化提供了额外的功能化潜力.其硬性丙烯菊酯核心有助于在医药化学应用中具有有利的约束特性.该化合物由于对湿气和空气的敏感性,通常在不热条件下处理,因此在高纯度条件下处理,确保合成工作流程的再生性.

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上下游产品

2-bromo-5H-pyrrolo[2,3-b]pyrazine (2-bromo-5-hydroxymethyl-5H-pyrrolo[2,3-b]pyrazin-7-yl)-methanol formaldehyd 2-cyclopropyl-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid cyclohexylamide N-(1-benzyl-4,4-dimethylpiperidin-3-yl)-2-cyclopropyl-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide 2-cyclopropyl-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (3-cyanophenyl)amide 2-phenoxy-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid cyclohexylamide

合成工艺路线路线简述

    📜(2-Bromo-7-Hydroxymethylpyrrolo[2,3-B]Pyrazin-5-yl)Methanol置于sodium Hydroxide,盐酸体系中,用 四氢呋喃,水 用作溶剂,以92%的收率获得(2-溴-5H-吡咯并[2,3-B]吡嗪-7-基)甲醇
    参考文献:Pyrrolopyrazines As Selective Spleen Tyrosine Kinase Inhibitors
    标题:Pyrrolopyrazines As Selective Spleen Tyrosine Kinase Inhibitors
    摘要:We Describe The Discovery Of Several Pyrrolopyrazines As Potent And Selective Syk Inhibitors And The Efforts That Eventually Led To The Desired Improvements In Physicochemical Properties And Human Whole Blood Potencies. Ultimately,Our Mouse Model Revealed Unexpected Toxicity That Precluded Us From Further Advancing This Series.
    Doi:10.1021/jm301720P

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