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-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-102125875-B 优先权日:2011-01-20 标 题 :Application of ferroceneimine cyclopalladium-phosphine adducts in the synthesis of unsymmetrical biaryl compounds
专利号:CN-102125875-A 优先权日:2011-01-20 标 题 :Application of ferroceneimine cyclopalladium-phosphine adducts in the synthesis of unsymmetrical biaryl compounds
专利号:CN-112537996-B 优先权日:2020-12-25 标 题 :Method for green synthesis of 2, 5-dibromo-1, 4-diiodobenzene intermediate
专利号:US-2024279179-A1 优先权日:2020-12-22 标题 :Synthesis and use of 1-benzyl-4-methyl-5-alkoxy-1,2,3,6-tetrahydropyridine derivative
[参考文献]: James Crawforth, Et Al. Tricyclic Pyridones As Functionally Selective Human Gabaa Alpha 2/3 Receptor-Ion Channel Ligands. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1679-82. [参考文献]: Richard Frenette, Et Al. Substituted 4-(2,2-Diphenylethyl)Pyridine-N-Oxides As Phosphodiesterase-4 Inhibitors: Sar Study Directed Toward The Improvement Of Pharmacokinetic Parameters. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3009-13.
合成参考文献
摘要:Cheng, Q.; Shen, X., Science of Synthesis: Knowledge Updates, (2025) 2. 摘要:Saha, D.; Aggarwal, T.; Sumii, Y.; Yadav, A. K.; Shibata, N., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.