5-氨基-2-三氟甲基吡啶置于亚硝酸特丁酯,Copper(Ll) Bromide体系中,用 乙腈 作为反应溶剂,化学反应 19.17H,以85%的收率获得产物5-溴-2-三氟甲基吡啶 参考文献:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia 标题:Selective Glyt1 Inhibitors: Discovery Of [4-(3-Fluoro-5-Trifluoromethylpyridin-2-yl)Piperazin-1-Yl][5-Methanesulfonyl-2-((S)-2,2,2-Trifluoro-1-Methylethoxy)Phenyl]Methanone (Rg1678),A Promising Novel Medicine To Treat Schizophrenia 摘要:The Glyt1 Transporter Has Emerged As A Key Novel Target For The Treatment Of Schizophrenia. Herein,We Report On The Optimization Of The 2-Alkoxy-5-Methylsulfonebenzoylpiperazine Class Of Glyt1 Inhibitors To Improve Herg Channel Selectivity And Brain Penetration. This Effort Culminated In The Discovery Of Compound 10A (Rg1678),The First Potent And Selective Glyt1 Inhibitor To Have A Beneficial Effect In Schizophrenic Patients In A Phase Ii Clinical Trial. DOI:10.1021/jm100210P
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-2024360125-A9 优先权日:2021-02-22 标 题 :2-substituted bicyclo[1.1.1]pentanes 发明人:MACMILLAN DAVID W; GARRY OLIVIA L; LIANG YUFAN; HEILMANN MICHAEL 权利人:UNIV PRINCETON 摘要:Provided herein are 2-substituted bicyclo[1.1.1]pentane (BCP) compounds, as well as methods of making the 2-substituted BCP compounds and methods of derivatizing the 2-substituted BCP compounds, particularly at the 2-position. The 2-substituted BCP compounds described herein are useful building blocks in the synthesis of a variety of products, including pharmaceuticals, polymers, liquid crystals, monolayers and supramolecular structures.
专利号:US-2009275616-A1 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
专利号:CN-105622491-A 优先权日:2014-10-28 标 题 :Synthesis of 6-trifluoromethylnicotinaldehyde
专利号:CN-112194616-A 优先权日:2019-07-08 标 题 :A kind of microwave synthesis method of 6-trifluoromethylpyridine carboxaldehyde
专利号:CN-109053553-A 优先权日:2018-10-16 标 题:Synthesis method of insecticide sulfoxaflor intermediate 3-[1-(methylthio)ethyl]-6(trifluoromethyl)pyridine
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