专利号:US-2013184465-A1 优先权日:2010-09-30 标 题:Process for the synthesis of thio-triazolo-group containing compounds 发明人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL 权利人:DOCHNAHL MAXIMILIAN; KEIL MICHAEL; GEBHARDT JOACHIM; VOGELBACHER UWE JOSEF; RACK MICHAEL; BASF SE 摘要:The present invention relates to a process using specific magnesium reagents for providing thio-triazolo group-containing compounds and for the synthesis of precursors therefor. The invention furthermore relates to intermediates and to their preparation.
专利号:US-7339065-B2 优先权日:2003-07-21 标题 :Design and synthesis of optimized ligands for PPAR 发明人:AVERY MITCHELL A; PERSHADSINGH HARRIHAR A 权利人:BETHESDA PHARMACEUTICALS INC; UNIV MISSISSIPPI 摘要:This invention provides new chemical entities useful for treating a variety of clinical disorders including those that are influenced by the activity of peroxisome proliferator activated receptors (PPAR). The structures of the compounds and methods to design, make and use the compounds are provided. Compounds and methods for administering therapeutic compositions comprising the compounds in cases of the disease psoriasis are provided. An exemplary compound having the formula compound is 5adamantan-2-yl-pentanoic acid {2-[4-(2,4-dioxo-thiazolidin-5-yl-methyl)-phenoxy]-ethyl}-methyl-amide is provided.
专利号:US-4446078-A 优先权日:1982-01-21 标 题 :Process for the preparation of α,α-difluoroalkyl-thiophenyl ketones 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl ketones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a carboxylic acid, a precursor or a derivative of this acid in the presence of boron trifluoride in such an amount that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-4552984-A 优先权日:1982-01-21 标题 :Process for preparation of α,α-difluoroalkoxy or α,.alpha. 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of alpha , alpha -difluoroalkoxy or alpha , alpha -difluoroalkylthiophenyl sulfones, in which a polyhaloalkoxybenzene or a polyhaloalkylthiobenzene is reacted with a sulfonic acid, a derivative or a precursor of this acid, in the presence of boron trifluoride in an amount such that the absolute pressure of the boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent. The resultant products are useful as intermediates in the synthesis of compounds having a phytosanitary (e.g., herbicidal) or pharmaceutical activity.
专利号:US-4438043-A 优先权日:1982-04-22 标题:Process for preparation of di- or trifluoromethoxyphenyl ketones or di- or trifluoromethylthiophenyl ketones 发明人:DESBOIS MICHEL 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the preparation of di- or trifluoromethoxyphenyl ketones or di- or trifluoromethylthiophenyl ketones, characterized in that, in a first stage, a di- or trihalomethoxybenzene or a di- or trihalomethylthiobenzene is reacted with a trihalomethylated aromatic or aliphatic compound in the presence of boron trifluoride in an amount such that the absolute pressure of boron trifluoride within the reaction vessel exceeds 1 bar, and in the presence of hydrofluoric acid as a solvent and in that, in a second stage, the product of the first stage is hydrolyzed. The resultant products are useful as intermediates in the synthesis of compounds having a pharmaceutical or phytosanitary (e.g., herbicidal) activity.
专利号:US-4621160-A 优先权日:1983-06-23 标题 :Process for the chlorination of aromatic derivatives 发明人:DESBOIS MICHEL; DISDIER CAMILLE 权利人:RHONE POULENC SPEC CHIM 摘要:A process for the chlorination of aromatic derivatives. The aromatic derivative is reacted with chlorine gas in liquid hydrofluoric acid. The products obtained are useful as intermediates for the synthesis of compounds having a plant-protecting or pharmaceutical activity.
[参考文献]: Enrico Baciocchi, Et Al. Synthesis Of Sulfoxides By The Hydrogen Peroxide Induced Oxidation Of Sulfides Catalyzed By Iron Tetrakis(Pentafluorophenyl)Porphyrin: Scope And Chemoselectivity. J Org Chem. 2004 May 14;69(10):3586-9. [参考文献]: G K Surya Prakash, Et Al. Preparation Of Tri- And Difluoromethylsilanes Via An Unusual Magnesium Metal-Mediated Reductive Tri- And Difluoromethylation Of Chlorosilanes Using Tri- And Difluoromethyl Sulfides, Sulfoxides, And Sulfones. J Org Chem. 2003 May 30;68(11):4457-63.
合成参考文献
摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 224. 摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 228. 摘要:Kleoff, M.; Omoregbee, K.; Zimmer, R., Science of Synthesis Knowledge Updates, (2018) 4, 220. 摘要:Barsegyan, Y. A.; Vil’, V. A.; Tomkinson, N. C. O.; Terent’ev, A. O., Science of Synthesis Knowledge Updates, (2022) 1, 266. 摘要:Koike, T.; Akita, M., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 568.