CAS: 774517-20-3; (S)-Quinuclidin-3-Yl (R)-1-Phenyl-3,4-Dihydroisoquinoline-2(1H)-Carboxylate

上下游产品

ethyl (R)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate (S)-quinuclidin-3-ol 1-phenyl-3,4-dihydroisoquinoline N-phenethylbenzamide (1S,3'S)-quinuclidin-3'-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monohydr°Chloride Solifenacin hydr°Chloride (1R,3'R)-quinuclidin-3'-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate monohydr°Chloride

📜1-苯基-3,4-二氢异喹啉置于sodium Tetrahydroborate,Sodium Hydride,Potassium Carbonate体系中,用 乙醇,二氯甲烷,甲苯 作为反应溶剂,化学反应 60.0H,反应生成 (1R,3S)-索利那新杂质2
参考文献:Synthesis And Antimuscarinic Properties Of Quinuclidin-3-Yl 1,2,3,4-Tetrahydroisoquinoline-2-Carboxylate Derivatives As Novel Muscarinic Receptor Antagonists
标题:Synthesis And Antimuscarinic Properties Of Quinuclidin-3-Yl 1,2,3,4-Tetrahydroisoquinoline-2-Carboxylate Derivatives As Novel Muscarinic Receptor Antagonists
摘要:In The Course Of Continuing Efforts To Develop Potent And Bladder-Selective Muscarinic M-3 Receptor Antagonists,Quinuclidin-3-Yl 1-Aryl-1,2,3,4-Tetrahydroisoquinoline-2-Carboxylate Derivatives And Related Compounds Were Designed As Conformationally Restricted Analogues Of Quinuclidin-3-Yl Benzhydrylcarbamate (8). Binding Assays With Rat Muscarinic Receptor Subtypes Revealed That The Quinuclidin-3-Yl 1-Aryl-1,2,3,4-Tetrahydroisoquinoline-2-Carboxylate Derivatives Showed High Affinities For The M3 Receptor,And Selectivity For The M3 Receptor Over The M-2 Receptor. Of These Derivatives,(+)-(1S,3'R)-Quinuclidin-3'-Yl 1-Phenyl-1,2,3,4-Tetrahydroisoquinoline-2-Carboxylate Monohydrochloride (9B) Exhibited Almost The Same Inhibitory Activity Against Bladder Contraction To That Of Oxybutynin (1),And More Than 10-Fold Selectivity For Bladder Contraction Versus Salivary Secretion,Demonstrating That 9B May Be Useful For The Treatment Of Symptoms Associated With Overactive Bladder Without Having Side Effects Such As Dry Mouth.
DOI:10.1021/jm050099Q

专利信息

专利号:US-7741489-B2
优先权日:2007-03-30
标题:Process for the synthesis of solifenacin
发明人：PUIG SERRANO JORDI; CAMPS PELAYO
权利人:MEDICHEM SA
摘要:The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.

专利号:US-2008242697-A1
优先权日:2007-03-30
标题 :Process for the synthesis of solifenacin

专利号:JP-2010523539-A
优先权日:2007-03-30
标 题:Improved synthesis of solifenacin

专利号:CA-2682381-A1
优先权日:2007-03-30
标题:An improved process for the synthesis of solifenacin

专利号:CN-101711248-A
优先权日:2007-03-30
标 题 :An improved process for the synthesis of solifenacin

专利号:KR-20100016116-A
优先权日:2007-03-30
标 题 :Advanced Synthesis of Solifenacin