CAS: 42864-78-8; 1-((3,4-Dimethoxyphenethyl)Amino)-3-(M-Tolyloxy)Propan-2-Ol Hydrochloride

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CAS号2186-25-6 1,2-环氧基-3-(3-甲基... | CAS号120-20-7 3,4-二甲氧基苯乙胺

📜间甲酚置于sodium Hydroxide体系中,用 乙醇,水 作为反应溶剂,化学反应 26.0H,反应生成 盐酸贝凡洛尔
参考文献:The Effective Direct Resolution Procedure For The Chiral Drug Bevantolol Hydrochloride
标题:The Effective Direct Resolution Procedure For The Chiral Drug Bevantolol Hydrochloride
摘要:The Solubility Of The Chiral Drug Bevantolol Hydrochloridel In Water And The Azeotropic Mixture Ethanol Water Has Been Investigated. It Was Found That Rac-1 Meets The Requirements Of Meyerhoffer'S Rule,So It Was Possible To Reduce The Ternary Diagram,Describing The Solubility Of 1,To A Pseudo Binary Form,Which Facilitates The Analysis Of Crystallization Processes Caused By Temperature Changes. On This Basis,The Effective And Robust Resolution Procedure Of Racemic Bevantolol Hydrochloride By A Preferential Crystallization Approach Has Been Realized Successfully. (C) 2016 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Tetasy.2016.03.012

专利信息

专利号:US-6387893-B1
优先权日:1999-09-30
标题 :Spirotricyclic substituted azacycloalkane derivatives and uses thereof
发明人：EVANS BEN E; HOFFMAN JACOB M; GILBERT KEVIN F; RITTLE KENNETH E
权利人:MERCK & CO INC
摘要:Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, 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-6232318-B1
优先权日:1998-11-12
标 题:Pyrimidinedione derivatives useful as alpha 1A adrenoceptor antagonists
发明人：NERENBERG JENNIE B; BOCK MARK G
权利人:MERCK & CO LTD
摘要:Novel pyrimidinedione 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-6326372-B1
优先权日:1999-09-30
标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
发明人：EVANS BEN E; GILBERT KEVIN F
权利人:MERCK & CO INC
摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts 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 typically 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: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-6436962-B1
优先权日:1999-09-30
标题:Arylhydantoin derivatives and uses thereof
发明人：HOFFMAN JACOB M; BOCK MARK G; DIPARDO ROBERT M; PAYNE LINDA S; PATANE MICHAEL A
权利人:MERCK & CO INC
摘要:Arylhydantoin derivatives and their pharmaceutically acceptable salts 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 typically 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.