📜3-氟苯腈置于1,3-二溴-5,5-二甲基海因,硫酸体系中,用 乙腈 作为反应溶剂,化学反应 8.0H,以90%的收率获得产物2-溴-5-氟苯腈 参考文献:Facile Synthesis Of 2-Bromo-3-Fluorobenzonitrile: An Application And Study Of The Halodeboronation Of Aryl Boronic Acids 标题:Facile Synthesis Of 2-Bromo-3-Fluorobenzonitrile: An Application And Study Of The Halodeboronation Of Aryl Boronic Acids 摘要:A Scaleable Synthesis Of 2-Bromo-3-Fluorobenzonitrile Via The Naome-Catalyzed Bromodeboronation Of 2-Cyano-6-Fluorophenylboronic Acid Was Developed. The Generality Of This Transformation Was Demonstrated Through The Halodeboronation Of A Series Of Aryl Boronic Acids. Both Aryl Bromides And Aryl Chlorides Were Formed In Good To Excellent Yields When The Corresponding Aryl Boronic Acid Was Treated With 1,3-Dihalo-5,5-Dimethylhydantoin And 5 Mol % Naome. DOI:10.1021/jo035184P
专利号:WO-0027817-A1 优先权日:1998-11-10 标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered uring flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:WO-0027827-A1 优先权日:1998-11-10 标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 权利人:MERCK & CO INC; NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 摘要:Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-6228870-B1 优先权日:1998-11-10 标 题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; PATANE MICHAEL A; SELNICK HAROLD G 权利人:MERCK & CO INC 摘要:Novel hydroxymethyl- and alkoxymethyl-oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-6235759-B1 优先权日:1998-10-29 标 题 :Dihydropyridinones and pyrrolinones useful as alpha 1A adrenoceptor antagonists 发明人:BARROW JAMES C; NANTERMENT PHILIPPE G; SELNICK HAROLD G 权利人:MERCK & CO INC 摘要:Novel dihydropyridinone and pyrrolinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-6319932-B1 优先权日:1998-11-10 标 题 :Oxazolidinones useful as alpha 1A adrenoceptor antagonists 发明人:NERENBERG JENNIE B; BOCK MARK G; SELNICK HAROLD G; PAYNE LINDA 权利人:MERCK & CO INC 摘要:Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:RU-2440355-C2 优先权日:2006-04-03 标 题:Method for synthesis of organoelement compounds
参考文献:10.1055/s-0036-1588303 摘要:Rossi R, Bellina F, Lessi M, Manzini C, Marianetti G. Direct (Hetero)arylation Reactions of (Hetero)arenes as Tools for the Step- and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets. Synthesis. 2016 Oct 11;48(22):3821–62. doi: 10.1055/s-0036-1588303.