CAS: 168267-99-0; 3-Fluoro-4-Methylbenzeneboronic Acid

相似化合物

903895-56-7 1621332-09-9 248270-25-9

上下游产品

Trimethyl borate 2-fluoro-4-bromotoluene 2-fluoro-4-iodotoluene

4-溴-2-氟甲苯置于正丁基锂,硼酸三异丙酯体系中,用 四氢呋喃,正己烷 用作溶剂,化学反应 1.5H,以82%的收率获得3-氟-4-甲基苯硼酸
参考文献:使用双功能接头进行click和suzuki偶联反应的模块化催化合成方法
标题:使用双功能接头进行click和suzuki偶联反应的模块化催化合成方法
摘要:稳定的苄基叠氮基硼酸酯1作为双功能接头的一个例子,允许在温和条件下将合成有价值的硼酸酯基序点击到其他分子上.叠氮基硼酸酯基序作为模块化构件的实用性已在使用顺序催化叠氮化物-炔烃环加成反应和suzuki偶联反应的药物样结构快速合成中得到证明.
Doi:10.1016/j.Tetlet.2010.05.104

专利信息

专利号:US-2020181095-A1
优先权日:2017-06-06
标题:Selective matrix metalloproteinase-13 inhibitors
发明人：FIELDS GREGG B; ROUSH WILLIAM R; CHOI JUN YONG; FUERST RITA
权利人:FLORIDA ATLANTIC UNIV BOARD OF TRUSTEES; SCRIPPS RESEARCH INST
摘要:We describe the use of comparative structural analysis and structure-guided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metalloproteinase 13 (MMP-13). We applied a three-step process, starting with a comparative analysis of the X-ray crystallographic structure of compound 5 in complex with MMP-13 with published structures of known MMP-13 inhibitor complexes followed by molecular design and synthesis of potent, but non-selective zinc-chelating MMP inhibitors (e.g., 10a and 10b). After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-10a, and 10b were binding within the MMP-13 active site, the Zn2+ chelating unit was replaced with non-chelating polar residues that bridged over the Zn2+ binding site and reach into a solvent accessible area. After two rounds of structural optimization, these design approaches led to small molecule MMP-13 inhibitors 10d and (S)-17b which bind within the substrate-binding site of MMP-13 and surround the catalytically active Zn2+ ion without chelating to the metal. These compounds exhibit at least 500-fold selectivity versus other MMPs.

专利号:US-8933018-B2
优先权日:2011-02-07
标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
发明人：GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA
权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC
摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.

专利号:RU-2136675-C1
优先权日:1993-09-22
标 题 :Derivatives of 3-(5-tetrazolylbenzyl)-aminopiperidine, methods of their synthesis and pharmaceutical composition on said

专利号:US-8846910-B2
优先权日:2006-08-22
标题:Matrix metalloproteinase inhibitors
发明人：SATTIGERI VISWAJANANI J; PALLE VENKATA P; KHERA MANOJ KUMAR; REDDY RANADHEER; TIWARI MANOJ KUMAR; SONI AJAY; RAUF ABDUL REHMAN ABDUL; JOSEPH SONY; MUSIB ARPITA; DASTIDAR SUNANDA G; SRIVASTAVA PUNIT KUMAR
权利人:RANBAXY LAB LTD
摘要:The present invention relates to β-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure β-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.