邻甲基苯腈置于n-溴代丁二酰亚胺(Nbs),过氧化苯甲酰体系中,用 四氯化碳,乙腈 作为反应溶剂,化学反应生成 Alpha-氰基-邻-苯乙腈 参考文献:Weiler-Feilchenfeld,H. Et Al.,Israel Journal Of Chemistry,1971,Vol. 9,P. 111-118 标题:Weiler-Feilchenfeld,H. Et Al.,Israel Journal Of Chemistry,1971,Vol. 9,P. 111-118
专利号:US-3954771-A 优先权日:1972-06-16 标题 :Process for the preparation of 2H-3-isoquinolones 发明人:GEERTS JEAN-PIERRE JULES; LINZ RAYMOND ARMAND 权利人:UCB SA 摘要:A process for the preparation of 2H-3-isoquinolones having the formula ##SPC1## n Wherein R 1 and R 2 are each hydrogen, halogen, lower alkyl, lower alkoxy, aryl, haloaryl, alkylaryl or alkoxyaryl; R 3 and R 4 are each hydrogen, lower alkyl, lower alkoxyalkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, or halo-aralkyl, which comprises cyclizing an N-formyl-2-phenyl-acetamide of the formula ##SPC2## n Wherein R 1 , R 2 , R 3 and R 4 have the same meaning as above, with a cyclodehydration agent. Said 2H-3-isoquinolones are useful as starting materials e.g. in the synthesis of 1,4-dihydro-1,4-etheno-isoquinolin-3(2H)-ones which are valuable chemotherapeutic agents in the treatment of disorders of the central nervous system, such as troubles of wakefulness, disorders of equilibrium and vertigo.
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:FR-2967673-A1 优先权日:2010-11-24 标题:SYNTHESIS OF N-HETEROCYCLES BY REDUCTIVE ALKYLATION OF CYAN DERIVATIVES
专利号:US-6358959-B1 优先权日:1999-01-26 标 题:Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists 发明人:BOCK MARK G; PATANE MICHAEL A; STEELE THOMAS G 权利人:MERCK & CO INC 摘要:Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) 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.
参考文献:10.1007/s00253-019-09915-8 摘要:Chen Z, Zhao J, Jiang S, Wei D. Recent research advancements on regioselective nitrilase: fundamental and applicative aspects. Applied Microbiology and Biotechnology. 2019 Jun 24;103(16):6393–405. doi: 10.1007/s00253-019-09915-8.