CAS: 98546-51-1; 4-(Methylthio)Phenylboronic Acid

上下游产品

CAS号104-95-0 4-溴硫代苯甲醚 | CAS号60822-47-1 4-Bromothioanisole | CAS号121-43-7 硼酸三甲酯 | CAS号5419-55-6 硼酸三异丙酯 | CAS号77-92-9 柠檬酸 | CAS号237429-33-3 4-巯基苯硼酸 | CAS号74-88-4 碘甲烷 | CAS号106-53-6 4-溴苯硫酚 | CAS号153312-70-0 (4-溴苯基硫代)二甲基叔丁基硅烷 | CAS号237429-34-4 4-[(dimethyl-te... | CAS号35371-03-0 4-碘茴香硫醚 | CAS号1016641-70-5 4,4,5,5-四甲基-2-(... | CAS号1073-72-9 4-(甲硫基)苯酚 | CAS号104-96-1 4-氨基茴香硫醚 | CAS号104-95-0 4-溴硫代苯甲醚 | CAS号329328-49-6 4-bromo-3-(4-me... | CAS号342651-54-1 2-methylsulfany... | CAS号14763-60-1 4-甲基磺酰苯酚 | CAS号166386-48-7 4-甲烷磺酰苯硼酸

4-溴茴香硫醚置于正丁基锂,硼酸三甲酯体系中,用 四氢呋喃 作为反应溶剂,化学反应 2.0H,以72%的收率获得产物4-甲硫基苯硼酸
参考文献:功能性芳族多磺酰氯及其掩蔽前体的合成.
标题:功能性芳族多磺酰氯及其掩蔽前体的合成.
摘要:含有苯乙酮和两个磺酰氯基团的功能性芳族双(磺酰氯)的合成,即3,5-双[4-(氯磺酰基)苯基]-1-乙酰苯(16),3,5-双(氯磺酰基)-1-苯乙酮(17)和3,5-双(4-(氯磺酰基)苯氧基)-1-苯乙酮(18)通过一系列反应进行,最后一步涉及s-(芳基)的定量氧化氯化-描述了n,N'-二乙基硫代氨基甲酸酯,烷基-或苄基硫代苯基作为磺酰氯的掩蔽的非反应性前体.相关的反应顺序用于合成芳族三磺酰氯1,1,1-三(4-氯磺酰苯基)乙烷(24).4-(氯磺酰基)苯氧基乙酸,2,2-双[[[[(4-(氯磺酰基)苯氧基乙酰基]氧基]甲基]-1,3-丙二酸酯(27),5,11,17,23-四(氯磺酰基)-25,26,27,28-四(乙氧羰基甲氧基)杯[4]芳烃(38),5,11,17,23,29,35-六(氯磺酰基)-37,38,39,40,41,42-六(乙氧羰基甲氧基)杯[6]芳烃(39),5
DOI:10.1021/jo001694X

专利信息

专利号:US-7244753-B2
优先权日:2002-07-29
标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D
权利人:NITROMED INC
摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:US-6825185-B2
优先权日:2000-12-21
标题:Substituted aryl compounds as novel cyclooxygenase-2 selective inhibitors, compositions and methods of use
发明人：KHANAPURE SUBHASH P; GARVEY DAVID S; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GASTON RICKY D
权利人:NITROMED INC
摘要:The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B 4 (LTB 4 ) receptor antagonists, leukotriene A 4 (LTA 4 ) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H 2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal toxicity or other toxicities; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

专利号:JP-2010222357-A
优先权日:2002-03-11
标题 :Intermediate compounds for the synthesis of aminoindazole derivatives

专利号:US-8841457-B2
优先权日:2010-11-15
标题:Process for cyclooxygenase-2 selective inhibitor
发明人：SHAH DHARMESH MAHENDRA; SOLANKI SANJAY AMRATLAL; JARIWALA VIRAL NARENDRA; VYAS ASHOK VASANTRAY; MISTRY ASHOKKUMAR BHIKHUBHAI
权利人:SHAH DHARMESH MAHENDRA; SOLANKI SANJAY AMRATLAL; JARIWALA VIRAL NARENDRA; VYAS ASHOK VASANTRAY; MISTRY ASHOKKUMAR BHIKHUBHAI; VIRDEV INTERMEDIATES PVT LTD
摘要:The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.

专利号:JP-5315287-B2
优先权日:2002-03-11
标 题 :Intermediate compounds for the synthesis of aminoindazole derivatives

专利号:US-7671085-B2
优先权日:2002-11-15
标 题 :Non-steroidal farnesoid X receptor modulators and methods for the use thereof
发明人：DOWNES MICHAEL R; EVANS RONALD M
权利人:SALK INST FOR BIOLOGICAL STUDI
摘要:The efficient regulation of cholesterol synthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. In accordance with the present invention, the identification of novel potent FXR activators is described. Two derivatives of invention compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds are useful as chemical tools to further define the physiological role of FXR as well as therapeutic leads for the treatment of diseases linked to cholesterol, bile acids and their metabolism and homeostasis.