CAS: 871329-82-7; (3-Fluoro-5-Hydroxyphenyl)Boronic Acid

上下游产品

3-fluoro-5-methoxyphenylboronic acid N-[2-(3,5-dimethyl-pyrazol-1-yl)-6-(3-fluoro-5-hydroxy-phenyl)-pyrimidin-4-yl]-acetamide {3-[(allylmethylamino)methyl]phenyl}-[4-(3-but-3-enyloxy-5-fluorophenyl)pyrimidin-2-yl]amine 4-(3-but-3-enyloxy-5-fluorophenyl)-2-chloropyrimidine 3-(4-amino-1-((1-phenyl-1H-benzo[d]imidazol-2-yl)methyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-5-fluorophenol

3-氟-5-甲氧基苯硼酸置于三溴化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,以430 Mg的收率获得产物3-氟-5-羟基苯基硼酸
参考文献: Heterocyclic Compounds And Methods Of Use[fr] Composés Hétérocycliques Et Procédés D'Utilisation
标题: Heterocyclic Compounds And Methods Of Use[fr] Composés Hétérocycliques Et Procédés D'Utilisation
摘要:本申请公开了抑制btk的化合物,抑制ρβKδ的化合物,以及既是btk又是pi3Kδ的双重抑制剂的化合物.还描述了合成这些抑制剂的方法,以及利用这些抑制剂治疗疾病的方法,其中抑制btk和pi3Kδ对患有该疾病的患者提供治疗益处.

专利信息

专利号:US-10017481-B2
优先权日:2012-03-17
标 题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC
权利人:POLYPHOR AG
摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.