📜2,4,6-三甲基吡啶,Lithium Trifluoromethanesulfonate置于氩,Fluorine体系中,用 乙腈 用作溶剂,以60%的收率获得1-氟-2,4,6-三甲基吡啶三氟甲烷磺酸盐 参考文献:Efficient Hydrolysis Of Dithioacetals By The N-Fluoro-2,4,6-Trimethylpyridinium Triflate-Water System 标题:Efficient Hydrolysis Of Dithioacetals By The N-Fluoro-2,4,6-Trimethylpyridinium Triflate-Water System 摘要:Dithioacetals Including 1,3-Dithianes And 1,3-Dithiolanes Are Efficiently Cleaved By The Title Reagent System To The Parent Carbonyl Compounds. The Cleavage Of Diprotected Symmetrical Alpha-Diketones And P-Phenylene-Diketones Gives Monoketones In Good Yields. Amide,1,3-Dioxolane,Disulfide,Ester,Ether,Hydroxy,Nitrile,Nitro,And Sulfide Functions Are Relatively Stable Under The Cleavage Conditions But Thiols Are Oxidized To Disulfides. Doi:10.1016/s0040-4020(01)80359-8
专利信息
专利号:US-12275733-B2 优先权日:2016-11-07 标 题:Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders 发明人:GRETZKE DIRK; RITZELER OLAF; HEINELT UWE; WEHNER VOLKMAR; SCHMIDT FRIEDEMANN 权利人:SANOFI SA 摘要:The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula (I), in which A, E, G, R1 to R6 and R10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.
专利号:US-10081610-B2 优先权日:2014-09-12 标题 :Efficient and scalable synthesis of 2-(1′h-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester and its structural analogs 发明人:SONG JIASHENG; ZHANG SUOMING; LI GUODONG; YANG LUQUING 权利人:ARIAGEN INC 摘要:Methods of synthesizing 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.
专利号:US-8558012-B2 优先权日:2009-03-02 标 题:2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative, production method thereof, and production method of monofluoromethyl group-containing compound using the same 发明人:SHIBATA NORIO 权利人:SHIBATA NORIO; NAGOYA INST TECHNOLOGY; TOSOH P TECH INC 摘要:A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R 1 , R 2 , R 3 , and R 4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.
专利号:US-6262254-B1 优先权日:1997-04-30 标 题 :8-fluoropurine compounds 发明人:BARRIO JORGE R; SATYAMURTHY NAGICHETTIAR; NAMAVARI MOHAMMAD; PHELPS MICHAEL E 权利人:UNIV CALIFORNIA 摘要:An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F 2 in He or other inert gas.
专利号:US-2017291881-A1 优先权日:2014-09-12 标 题:Efficient and scalable synthesis of 2-(1'h-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester and its structural analogs
专利号:CN-107001350-B 优先权日:2014-09-12 标题 :Efficient and scalable synthesis of methyl 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylate and its structural analogs
摘要:McMurtrey, K. B.; Sanford, M. S., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 559. 摘要:McMurtrey, K. B.; Sanford, M. S., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 560. 摘要:van der Puyl, V.; Shenvi, R. A., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 654. 摘要:van der Puyl, V.; Shenvi, R. A., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 647. 摘要:van der Puyl, V.; Shenvi, R. A., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 643.