O-Bromobenzenediazonium置于alkali体系中,化学反应生成2-溴茴香硫醚 参考文献:Van Hove,Bulletin De La Classe Des Sciences,Academie Royale De Belgique,1926,Vol. <5>12,P. 940,941; 标题:Van Hove,Bulletin De La Classe Des Sciences,Academie Royale De Belgique,1926,Vol. <5>12,P. 940,941;
专利号:US-5908935-A 优先权日:1996-09-18 标 题:Process for the preparation of 1-Acyl-4-arylpiperidines 发明人:BRIEDEN WALTER; LOETSCHER DIDIER; NAUGHTON ANDREW 权利人:LONZA AG 摘要:1-Acyl-4-arylpiperidines of the general formula: ##STR1## wherein R 1 is an aryl group optionally substituted by one or more C 1-6 -alkyl groups, C 1-6 -alkoxy groups, benzyloxy groups or C 1-6 -alkylthio groups and/or one or more fluorine atoms, and R 2 is a C 1-6 -alkyl group, a C 1-6 -alkoxy group, an optionally substituted aryl group, alkylaryl group or a benzyloxy group optionally substituted on the phenyl radical. The 1-acyl-4-arylpiperidines of formula I are prepared by reacting an arylmagnesium halide with a 1-acylpyridinium halide, obtainable from pyridine and an acyl halide, in the presence of a copper compound to give the corresponding 1-acyl-4-aryl-1,4-dihydropyridine, and hydrogenating the latter. The 1-acyl-4-arylpiperidines are intermediates in the synthesis of pharmaceutical active ingredients, for example, neurokinin receptor antagonists.
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-6495713-B2 优先权日:2001-01-17 标 题 :Synthesis of ketosulfone esters 发明人:CHEN CHENG YI; CHEN WEIRONG; O'SHEA PAUL; TAN LUSHI; TILLYER RICHARD; XU FENG; DAGNEAU PHILIPPE 权利人:MERCK & CO INC 摘要:This invention encompasses a process for making a compound of Formula A n These compounds are intermediates useful in the preparation of certain non-steroidal anti-inflammnatory agents.
专利号:US-2002143205-A1 优先权日:2001-01-17 标 题:Synthesis of ketosulfone esters
专利号:CA-2433927-A1 优先权日:2001-01-17 标 题 :Synthesis of ketosulfone esters
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
[参考文献]: Youngmin Kim, Et Al. Sulfonium Boranes For The Selective Capture Of Cyanide Ions In Water. Angew Chem Int Ed Engl. 2009;48(27):4957-60.
合成参考文献
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 73. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 989. 摘要:Lattanzi, A., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 1000.