专利号:US-9000209-B2 优先权日:2011-07-22 标题:Method of regioselective synthesis of substituted benzoates 发明人:KRAUS GEORGE A 权利人:KRAUS GEORGE A; UNIV IOWA STATE RES FOUND INC 摘要:A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an unactivated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carried out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the unactivated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomeric meta-substituted impurity.
专利号:US-9856275-B2 优先权日:2013-02-12 标 题:Synthesis and use of fluorinated compounds 发明人:MOLANDER GARY ALAN; ARGINTARU OANA ANDREEA 权利人:UNIV PENNSYLVANIA 摘要:The invention is directed to the preparation of fluorinated compounds and their use in organic synthesis. In particular, the invention is directed to methods of reacting compounds of structure with R f —CHâ•?N 2 or (CF 3 ) 2 Câ•?N 2 to form a perfluoroalkylate or -arylated compounds, and products derived from these reactions, where X, Y B , and R f are described herein.
专利号:US-2011183958-A1 优先权日:2008-10-17 标 题 :Azetidine derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:POWELL DAVID; TRANMER GEOFFREY K 权利人:MERCK FROSST CANADA LTD 摘要:Azetidine derivatives of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer; liver steatosis; and non-alcoholic steatohepatitis.
专利号:US-2014288324-A1 优先权日:2011-07-22 标 题:Method of regioselective synthesis of substituted benzoates
专利号:CN-112679346-A 优先权日:2021-01-22 标题 :A kind of method based on catalyzed synthesis of methyl p-tert-butyl benzoate based on deep eutectic solvent
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.
[参考文献]: Guoqing Zhang, Et Al. Polymorphism And Reversible Mechanochromic Luminescence For Solid-State Difluoroboron Avobenzone. J Am Chem Soc. 2010 Feb 24;132(7):2160-2.
合成参考文献
摘要:Schobert, R.; Hölzel, C.; Barnickel, B., Science of Synthesis, (2010) 47, 64. 摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 299. 摘要:Mitsudo, K.; Suga, S., Science of Synthesis, (2020) , 450. 摘要:Schiltz, P.; Gosmini, C., Science of Synthesis: Special Topics, (2021) 1, 97. 摘要:Folgueiras-Amador, A. A.; Wirth, T., Science of Synthesis: Flow Chemistry in Organic Synthesis, (2018) 1, 163.