CAS: 245762-35-0; 5-Fluoro-2,3-Dihydrobenzofuran

相似化合物

496-16-2 1072153-64-0 175203-20-0

上下游产品

CAS号24410-59-1 5-氟苯并呋喃 | CAS号371-41-5 4-氟苯酚 | CAS号59769-37-8 1-(2,2-Diethoxy... | CAS号42933-43-7 5-氨基-2,3-二氢苯并[b]呋喃 | CAS号245762-37-2 5-氟-2,3-二氢苯并呋喃-7-醇 | CAS号245762-36-1 5-Fluoro-2,3-di...

2,3-二氢苯并呋喃置于盐酸,Tetrafluoroboric Acid,Palladium 10% On Activated Carbon,氢气,硝酸,三氟乙酸,Sodium Nitrite体系中,用 四氢呋喃,乙醇,水 用作溶剂,-15.0~20.0 °C,413.7 Kpa 条件下,反应 23.5H,反应生成5-氟-2,3-二氢苯并[b]呋喃
参考文献:Discovery And Structure-activity Relationship Of Novel 2,3-Dihydrobenzofuran-7-Carboxamide And 2,3-Dihydrobenzofuran-3(2H)-One-7-Carboxamide Derivatives As Poly(Adp-Ribose)Polymerase-1 Inhibitors
标题:Discovery And Structure-activity Relationship Of Novel 2,3-Dihydrobenzofuran-7-Carboxamide And 2,3-Dihydrobenzofuran-3(2H)-One-7-Carboxamide Derivatives As Poly(Adp-Ribose)Polymerase-1 Inhibitors
摘要:Novel Substituted 2,3-Dihydrobenzofuran-7-Carboxamide (Dhbf-7-Carboxamide) And 2,3-Dihydrobenzofuran-3(2H)-One-7-Carboxamide (Dhbf-3-One-7-Carboxamide) Derivatives Were Synthesized And Evaluated As Inhibitors Of Poly(Adp-Ribose)Polymerase-1 (Parp-1). A Structure-Based Design Strategy Resulted In Lead Compound 3 (Dhbf-7-Carboxamide; Ic50 = 9.45 Mu M). To Facilitate Synthetically Feasible Derivatives,An Alternative Core Was Designed,Dhbf-3-One-7-Carboxamide (36,Ic50 = 16.2 Mu M). The Electrophilic 2-Position Of This Scaffold Was Accessible For Extended Modifications. Substituted Benzylidene Derivatives At The 2-Position Were Found To Be The Most Potent,With 3',4'-Dihydroxybenzylidene 58 (Ic50 = 0.531 Mu M) Showing A 30-Fold Improvement In Potency. Various Heterocycles Attached At The 4'-Hydroxyl/4'-Amino Of The Benzylidene Moiety Resulted In Significant Improvement In Inhibition Of Parp-1 Activity (E.G.,Compounds 66-68,70,72,And 73; Ic50 Values From 0.718 To 0.079 Mu M). Compound 66 Showed Selective Cytotoxicity In Brca2-Deficient Dt40 Cells. Crystal Structures Of Three Inhibitors (Compounds (-)-13C,59,And 65) Bound To A Multidomain Parp-1 Structure Were Obtained,Providing Insights Into Further Development Of These Inhibitors.
Doi:10.1021/jm5002502

专利信息

专利号:US-2011137038-A1
优先权日:2006-11-09
标题 :Synthesis of selected stereoisomers of certain substituted alcohols
发明人：HARMS ARTHUR E
权利人:HARMS ARTHUR E
摘要:A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.

专利号:US-2008114172-A1
优先权日:2006-11-09
标 题 :Synthesis of Selected Stereoisomers of Certain Substituted Alcohols

专利号:EP-2086921-A2
优先权日:2006-11-09
标 题:Synthesis of selected stereoisomers of certain substituted alcohols

专利号:JP-2008517929-A
优先权日:2004-10-21
标题:Asymmetric synthesis of dihydrobenzofuran derivatives

专利号:WO-2008060799-A2
优先权日:2006-11-09
标题:Synthesis of selected stereoisomers of certain substituted alcohols