CAS: 63659-17-6; 2-[[4-[2-(Cyclopropylmethoxy)Ethyl]Phenoxy]Methyl]Oxirane

上下游产品

4-[2-(cyclopropylmethoxy)-ethyl]-phenol epichlorohydrin 1,2-Epoxy-3-bromopropane 1-allyloxy-4-(2-cyclopropylmethoxyethyl)benzene

2-(4-苯甲氧基苯基)乙醇置于palladium On Activated Charcoal Sodium Hydroxide,氢气,Sodium Hydride体系中,用 四氢呋喃,水 作为反应溶剂,25.0~60.0 °C,344.73 Kpa 条件下,反应 30.0H,反应生成 1-{4-[2-(环丙基甲氧基)-乙基]-苯氧基}-2,3-环氧丙烷
参考文献:Synthesis Of A Series Of Compounds Related To Betaxolol,A New .Beta.1-Adrenoceptor Antagonist With A Pharmacological And Pharmacokinetic Profile Optimized For The Treatment Of Chronic Cardiovascular Diseases
标题:Synthesis Of A Series Of Compounds Related To Betaxolol,A New .Beta.1-Adrenoceptor Antagonist With A Pharmacological And Pharmacokinetic Profile Optimized For The Treatment Of Chronic Cardiovascular Diseases
摘要:A Series Of Para-Substituted Phenoxypropanolamines Has Been Synthesized And Tested For Beta-Adrenoceptor Blocking Activity. Some Derivatives (8,11,12,20,21) Exhibited Greater In Vitro Potency Than The Reference Drugs Metoprolol And Propranolol. This Series,In Contrast To Propranolol But Similar To Metoprolol,Possesses Cardioselectivity. The 3-[p-[(Cycloalkylmethoxy)Ethyl]Phenoxy]-1-Substituted-Amino-2-Prop Anol Derivatives 8 (Cyclopropylmethoxyethyl: Betaxolol) And 11 (Cyclobutylmethoxyethyl) Produced Antihypertensive Effects In Spontaneously Hypertensive Rats. Betaxolol (Kerlon,8) Was Found To Exhibit An Appropriate Preclinical Pharmacological And Human Pharmacokinetic Profile (Elevated Oral Bioavailability And Prolonged Plasma Half-Life) For The Treatment Of Chronic Cardiovascular Diseases Such As Hypertension And Angina.
DOI:10.1021/jm00389A008

专利信息

专利号:US-2021154202-A1
优先权日:2018-04-17
标 题:Synthesis of dentimol, an antiglaucoma drug
发明人：LANCINA MICHAEL; WANG JUAN; YANG HU
权利人:UNIV VIRGINIA COMMONWEALTH
摘要:Compounds, comprising a selective β-blocker coupled to a PAMAM dendrimer via a flexible spacer, and compositions containing the compounds, are provided. Methods of making and using the compounds and compositions for the treatment of glaucoma and other maladies are also provided.