三氟甲氧基苯置于溴,铁粉体系中,化学反应 16.0H,以83.8%的收率获得产物对溴三氟甲氧基苯 参考文献:C-Aryl Glucoside Derivatives,Preparation Process And Pharmaceutical Use Thereof 标题:C-Aryl Glucoside Derivatives,Preparation Process And Pharmaceutical Use Thereof 摘要:C-芳基葡萄糖苷衍生物,其制备方法和药用用途已被披露.具体来说,公开了由式(I)表示的c-芳基葡萄糖苷衍生物,其中每个取代基在申请中定义,其药学上可接受的盐或立体异构体,它们的制备方法,以及含有这些衍生物的药物组合物以及它们作为治疗剂的用途,特别是作为钠依赖性葡萄糖协同转运蛋白(Sglt)-1抑制剂.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:US-4157344-A 优先权日:1978-01-16 标题 :Preparation of aryl trifluoromethyl ethers 发明人:FEIRING ANDREW E 权利人:DU PONT 摘要:A one-step process for the synthesis of aryl trifluoromethyl ethers by reacting phenol or certain substituted phenols with a perhalomethane and hydrogen fluoride is provided. The compounds produced by the process of this invention are useful intermediates in the production of dyestuffs and pharmaceuticals.
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-6441189-B1 优先权日:2000-03-31 标 题 :Process for the preparation of matrix metalloproteinase inhibitors 发明人:BAILEY ANNE E; HILL DAVID R; HSIAO CHI-NUNG W; KURUKULASURIYA RAVI; WITTENBERGER STEVE; MCDERMOTT TODD; MCLAUGHLIN MAUREEN A 权利人:ABBOTT LAB 摘要:The instant invention provides a process for the synthesis of matrix metalloproteinase inhibitors.
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.
摘要:Bolduc, T. G.; Thomson, B.; Sammis, G. M., Science of Synthesis, (2020) , 390. 摘要:Ghosh, I., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 418. 摘要:Yerien, D. E.; Barata-Vallejo, S.; Postigo, A., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 9.