CAS: 51446-30-1; 2-Fluoro-5-Hydroxybenzoic Acid

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CAS号672931-28-1 2-氟-5-甲氧基苯乙腈 | CAS号161643-29-4 (2-氟-5-甲氧基苯基)甲醇 | CAS号91319-42-5 2-(溴甲基)-1-氟-4-甲氧基苯

📜2-氟-5-羟基苯甲酸甲酯置于lithium Hydroxide Monohydrate体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 16.0H,以91%的收率获得产物2-氟-5-羟基苯甲酸
参考文献:平行合成策略在联苯酰基酰基磺酰胺作为高效和选择性na V 1.7抑制剂的发现中的应用
标题:平行合成策略在联苯酰基酰基磺酰胺作为高效和选择性na V 1.7抑制剂的发现中的应用
摘要:大多数有效的和选择性的hna V 1.7抑制剂具有常见的药理学特征,包括杂芳基磺酰胺头基和亲脂性芳族尾基.最近,已经出现了类似的芳香族尾基与酰基磺酰胺头基结合的报道,酰基磺酰胺赋予了相对于hna V的选择性水平1.5与杂芳基磺酰胺相当.从满足亲脂性尾部中选定药理学要求的市售羧酸开始,采用平行合成方法快速反应生成衍生的酰基磺酰胺.精心制作了该文库中的联芳基酰基磺酰胺,优化了效价和选择性,并关注了理化性质.所得的新的铅是有效的,配体和亲脂性的,并且在hna V 1.5上具有选择性.代表性的铅36证明了在鼠类中对其他人类na V同工型的选择性和非常好的药代动力学.与已知的杂芳基磺酰胺抑制剂相比,本文报道的联芳基酰基磺酰胺还可以提供adme优势.
DOI:10.1021/acs.Jmedchem.6B00425

专利信息

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.