三乙胺置于氢氧化钾,乙酸酐体系中,用 四氯化碳 作为反应溶剂,以79%的收率获得产物6-羟基烟酸 参考文献:Process For The Production Of 2-Hydroxypyridines From 2-Pyridine 标题:Process For The Production Of 2-Hydroxypyridines From 2-Pyridine 摘要:生产具有以下化学式的2-羟基吡啶的过程:##str1## 从具有以下化学式的2-吡啶羧酸-N-氧化物开始:##str2## 其中r为h,一个--Cooh基团,具有1至8个碳原子的烷基基团或芳基基团,N代表1至4之间的数字.在三级胺的存在下,使用低级脂肪羧酸酐将n-氧化物转化.然后水解转化产物.
专利号:US-6258323-B1 优先权日:1998-11-16 标题:Apparatus and method used in multiple, simultaneous synthesis of general compounds 发明人:HORMANN ROBERT EUGENE; GILBERT DARYL EUGENE; SIOMA EDWARD MICHAEL 权利人:ROHM & HAAS 摘要:The apparatus and method of the present invention provides for conducting simultaneous multiple synthesis of general compounds, which often takes place under varied uneven conditions requiring heating, cooling, agitation, reagent/solvent additions to the reactor contents at each reaction vessel location, supply and maintenance of inert atmosphere and means to facilitate the reflux of the reactor contents. Thus, it becomes necessary to monitor and control the reaction conditions during the simultaneous multiple synthesis of general compounds. The apparatus allows the user to connect various independently controlling and conveying means to each reaction vessel through multiple ports provided on a stopper mounted on each reaction vessel. The apparatus of the present invention permits user to readily access the reaction vessels without interrupting the reactions occurring in the adjacent reaction vessels. The unique geometry and shape of the stopper allows positioning of multiple ports, while still providing the stopper with a compact size. As a result, a large array of reaction vessels can be accommodated in the device of the present invention without significantly increasing the overall size of the apparatus. Some of the general compounds that can be readily synthesized by the apparatus and the method of the present invention include inorganic compounds as well as organic compounds, such as oligomers, polymers, agricultural chemicals, drugs, peptides and oligonucleotides.
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.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
专利号:US-7151112-B1 优先权日:2001-09-04 标题:Pharmaceutical uses and synthesis of nicotinamides 发明人:CUTSHALL NEIL S; JEFFREY SCOTT C 权利人:UCB SA 摘要:This invention is directed to methods of using a compound of the formula n nand pharmaceutically acceptable salts thereof, wherein n, X, R 1 and R 2 are disclosed herein, for treating inflammatory events in an animal subject.
专利号:US-4349681-A 优先权日:1979-12-24 标题:2-Amino-3-chloro-5-trifluoromethylpyridine 发明人:YOKOMICHI ISAO; HAGA TAKAHIRO; NAGATANI KUNIAKI; NAKAJIMA TOSHIO 权利人:ISHIHARA MINING & CHEMICAL CO 摘要:A novel compound, 2-amino-trifluoromethyl-halogenopyridine, is provided, which is prepared by amination of a 2-halogeno-trifluoromethyl-halogenopyridine or by halogenation of 2-amino-trifluoromethylpyridine. This compound is useful as an intermediate for synthesis of agricultural chemicals and medicines.
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