CAS: 140924-50-1; 1,4-Bis((R)-((1S,2S,4S,5R)-5-Ethylquinuclidin-2-yl)(6-Methoxyquinolin-4-yl)Methoxy)Phthalazine

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CAS号4752-10-7 1,4-二氯酞嗪 | CAS号522-66-7 氢化奎宁

1,4-二氯酞嗪,氢化奎宁置于氢氧化钾,Potassium Carbonate体系中,用 甲苯 用作溶剂,化学反应 14.0H,以68%的收率获得氢化奎宁 1,4-(2,3-二氮杂萘)二醚
参考文献:Syntheses And Crystal Structures Of The Cinchona Alkaloid Derivatives Used As Ligands In The Osmium-Catalyzed Asymmetric Dihydroxylation Of Olefins
标题:Syntheses And Crystal Structures Of The Cinchona Alkaloid Derivatives Used As Ligands In The Osmium-Catalyzed Asymmetric Dihydroxylation Of Olefins
摘要:Experimental Procedures For The Preparation Of Two Classes Of Derivatives Of The Cinchona Alkaloids Dihydroquinine And Dihydroquinidine Are Described. Ligands (Dhq)2-Phal,La,And (Dhqd)2-Phal,2A,Are Conveniently Synthesized In Good Yield By The Reaction Of The Corresponding Alkaloid With 1,4-Dichlorophthalazine In The Presence Of K2Co3 And Koh In Refluxing Toluene. Derivatives Dhq-Phn,Lb,And Dhqd-Phn,2B,Are Prepared Through An Ullmann-Type Coupling Between The 9-0-Alkaloid Sodium Alkoxide And 9-Iodophenanthrene In The Presence Of Cui And Pyridine. Crystal Structures For Derivatives 2A And 2B Are Also Presented. These Four Alkaloid Derivatives Serve As Highly Enantioselective Ligands For The Osmium Tetraoxide Catalyzed Asymmetric Dihydroxylation (Ad) Of Olefins.
Doi:10.1021/jo00056A015

专利信息

专利号:US-2005239767-A1
优先权日:2003-10-28
标题 :Intermolecular SNAr of the heterocycle-activated nitro and fluoro groups-application in the synthesis of polyazamacrocyclic ligands
发明人：CHAN MICHAEL K; FEKNER TOMASZ
权利人:CHAN MICHAEL K; FEKNER TOMASZ
摘要:A new class of tetracylic benzimidazole compounds and derivatives thereof. Additionally provided is a synthetic route for the generation of these and related compounds via Intramolecular Aromatic Nucleophilic Substitution (S N Ar) of the Benzimidazole-Activated Nitro Groups. Additionally, a facile route for the generation of novel phenol species as thermal decomposition of compounds the S N Ar product, which occurs at high temperature resulting in cleavage of the ether linkage and formation of a vinyl group and phenol is provided. Also provided are methods of using the compounds described herein in the treatment HIV.

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:WO-0027816-A1
优先权日:1998-11-10
标题:Oxazolidinones useful as alpha 1a adrenoceptor antagonists
发明人：SELNICK HAROLD G; BARROW JAMES
权利人:MERCK & CO INC; SELNICK HAROLD G; BARROW JAMES
摘要:(4-Aryl-4-hydroxypiperidinyl) alkylcarbamoyl 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-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.