CAS: 882-09-7; 2-(4-Chlorophenoxy)-2-Methylpropanoic Acid

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CAS号637-07-0 氯贝特 | CAS号2052-01-9 2-溴代异丁酸 | CAS号106-48-9 对氯苯酚 | CAS号31637-97-5 依托贝特 | CAS号57-15-8 三氯叔丁醇 | CAS号67-66-3 氯仿 | CAS号67-64-1 丙酮 | CAS号600-00-0 2-溴-2-甲基丙酸乙酯 | CAS号1193-00-6 对氯苯酚钠 | CAS号63394-05-8 普拉贝脲 | CAS号105377-53-5 2-[bis(2-hydrox... | CAS号106-48-9 对氯苯酚 | CAS号5542-60-9 2-(4-氯丙氧基)-2-甲基丙酰氯 | CAS号637-07-0 氯贝特 | CAS号93010-95-8 2-(4-chlorophen... | CAS号47662-72-6 2-(diethylamino... | CAS号55162-41-9 2-(4-氯苯氧基)-2-甲基丙酸甲酯 | CAS号5658-61-7 2-(4-氯苯氧基)-2-甲基丙酰胺 | CAS号57966-38-8 2-(2,2-dimethyl... | CAS号61887-14-7 phenyl 2-(4-chl...

对氯苯酚置于potassium Carbonate,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 16.17H,反应生成 氯贝酸
参考文献:新型,有效,选择性,口服生物利用腺苷a 2A受体拮抗剂的设计,合成及其生物学评价
标题:新型,有效,选择性,口服生物利用腺苷a 2A受体拮抗剂的设计,合成及其生物学评价
摘要:我们对7位-甲氧基-4-吗啉代-苯并噻唑衍生物在2位上具有特征性的芳氧基-2-甲基丙酰胺部分的初步构效关系研究导致将化合物25鉴定为有效且选择性的a 2A腺苷受体(a 2A Ador)具有合理adme和药代动力学特性的拮抗剂.但是,固有溶解性差和口服生物利用度低至中等,使得该系列不适合进一步开发.使用基于结构的药物设计方法进行的进一步优化导致发现了有效和选择性的腺苷a 2A受体拮抗剂在苯并噻唑支架的2位带有取代的1-甲基环己基甲酰胺基,具有更好的溶解度和口服生物利用度.化合物41和49在体外adme特性方面表现出许多积极的特性.两种化合物在大鼠中均表现出非常好的药代动力学性质,口服生物利用度分别为63%和61%.此外,化合物49在帕金森氏病的6-Ohda损伤的大鼠模型中显示出口服功效.
DOI:10.1021/acs.Jmedchem.6B01584

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:WO-2008150031-A1
优先权日:2007-06-08
标题:Inhibitor of biosynthesis of plant hormone auxin, chemical plant regulator comprising the inhibitor as active ingredient, herbicidal agent, and use thereof
发明人：SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO
权利人:RIKEN; SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO
摘要:The first object is to provide an inhibitor of the synthesis of endogenous auxin. The second object is to provide a plant growth inhibitor or a herbicidal agent utilizing the auxin biosynthesis inhibitor. Thus, disclosed are: a method for screening a candidate for an auxin biosynthesis inhibitor capable of inhibiting the expression of an auxin-inducible gene, by adding each of candidate compounds for the auxin inhibitor to a plant; a method for selecting a compound capable of actually inhibiting the auxin synthesis in a plant, by adding each of candidate compounds to the plant, disrupting the plant and then measuring the amount of endogenous auxin; and a method for selecting a compound capable of inhibiting the production of indolpyruvic acid in the presence of a tryptophan deaminase and tryptophan which are prepared in advance. More specifically disclosed are: an auxin biosynthesis inhibitor comprising AVG, AOA, AOIBA, L-AOPP or an analogue thereof; and a plant growth regulator or a herbicidal agent comprising the compound as an active ingredient.

专利号:US-2005004225-A1
优先权日:2003-04-16
标题:Oxidoreductase inhibitors and methods of screening and using thereof
发明人：BALENDIRAN GANESARATNAM K
摘要:The present invention relates to 1) the design and synthesis of analogs to glutathione conjugates which bind to or interact with aldose reductase (AR) through unique conformations that are distinctly different from the substrates and inhibitors of AR which are members of sugar metabolism; 2) the screening of the analogs to identify those that interact with or inhibit or enhance the activity of AR; and 3) the use of AR ligands, AR inhibitors (AR antagonsits) or AR enhancer (AR agonists) in the detection of AR activity, the modulation of AR activity, and the treatment of conditions in a subject in need of modulating AR activity. Such conditions include but not limited to cardiovascular disease, diabetes, artheriosclerosis, cancer, neoplasm, obesity, cataract, retinopathy, keratopathy, nephropathy, neurosis, thrombosis, faulty union of corneal injury and neuropathy. Examples of the treatment include the use of fibrates as AR inhibitors to treat these conditions.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-4897475-A
优先权日:1988-02-05
标 题:Process for synthesis of 5α-cholest-8(14)-en-3β-ol-15-one and other 15-oxygenated sterols
发明人：SCHROEPFER JR GEORGE J; WILSON WILLIAM K; WANG KER-SHI; KISIC ALEMKA
权利人:UNIV RICE WILLIAM M
摘要:A process for preparing 15-oxygenated sterols, such as 3β-hydroxy-5α-cholest-8(14)-ene-15 one, comprising converting 7-dehydrocholesterol to 3β-benzoyloxycholesta-5,7-diene, converting the 3β-benzoyloxycholesta-5,7-diene to a 3β-benzoyloxy-5-cholesta-7,14-diene, converting the 3β-benzoyloxy-5-cholesta-7,14-diene to a 3β-benzoyloxy-14α, 15α-epoxy-5-cholest-7-ene and converting the 3β-benzoyloxy-14α, 15α-epoxy-5-cholest-7-ene to a 15-oxygenated sterol. Preferably, the 3β-benzoyloxy-cholesta-5,7-diene is converted to a 3β-benzoyloxy-5-cholesta-7,14-diene by (i) contacting 3β-benzoyloxy-cholesta-5,7-diene, in a solvent at a temperature of at most about -55° C., with HCl at a concentration of at least about 2.0 M for a time sufficient to convert the 3β-benzoyloxycholesta-5,7-diene to a 3β-benzoyloxy-5-cholesta-7,14-diene; (ii) neutralizing the resultant reaction mixture with a base to prevent formation of a significant amount of 3β-benzoyloxy-5-cholesta-8,14-diene; and (iii) recovering the 3β-benzoyloxy-5-cholesta-7,14-diene.

专利号:US-11078093-B2
优先权日:2017-06-30
标 题 :Surfactant-assisted synthesis of surface-functionalized nanoparticle-polymer electrospun composites
发明人：CWIERTNY DAVID; MYUNG NOSANG; PETER KATHERINE T; PARKIN GENE FRANCIS
权利人:UNIV CALIFORNIA; UNIV IOWA RES FOUND
摘要:A method is disclosed for synthesizing nanofilters for water treatment. The method includes: dispersing an active binding agent in an organic solvent solution to create a suspension of the active binding agent and the solution of the solvent; dissolving an organic polymer resin and an anionic surfactant in the suspension of the active binding agent and the solvent solution to create a sol gel; and electrospinning the sol gel to form electrospun nanofiber composites with embedded, surface-active nanoparticles.