CAS: 101048-76-4; 2-Fluoro-4-Formylbenzonitrile

相似化合物

176508-81-9 222978-02-1 3906-87-4

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CAS号222978-02-1 2-氟-4-(羟甲基)苄甲腈 | CAS号2591-86-8 1-甲酰哌啶 | CAS号105942-08-3 4-溴-2-氟苯腈 | CAS号440105-58-8 4-(dibromomethy... | CAS号222978-03-2 4-氰基-3-氟苄溴 | CAS号64-17-5 乙醇 | CAS号1634-04-4 甲基叔丁基醚 | CAS号452-74-4 3-氟-4-溴甲苯 | CAS号85070-67-3 2-氟-4-甲基苯腈 | CAS号222978-01-0 4-溴-3-氟苄醇 | CAS号222978-26-9 2-fluoro-4-[hyd... | CAS号222978-02-1 2-氟-4-(羟甲基)苄甲腈

📜2-氟-4-甲基苯腈置于n-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,十二/十四烷基二甲基氧化胺体系中,用 四氯化碳,二氯甲烷,二甲基亚砜 用作溶剂,化学反应 13.0H,反应生成2-氟-4-甲酰基苯甲腈
参考文献:A Fluorine Scan Of The Phenylamidinium Needle Of Tricyclic Thrombin Inhibitors: Effects Of Fluorine Substitution On Pkaand Binding Affinity And Evidence For Intermolecular C-f⋯cn Interactions
标题:A Fluorine Scan Of The Phenylamidinium Needle Of Tricyclic Thrombin Inhibitors: Effects Of Fluorine Substitution On Pkaand Binding Affinity And Evidence For Intermolecular C-f⋯cn Interactions
摘要:三环凝血酶抑制剂的苯基氨定针中的氢原子与酶选择性口袋 S1 底部的 Asp189 发生相互作用,系统地将这些氢原子替换为氟原子,试图通过降低 Pka 值来改善药代动力学特性.F-替代后,Pka 值以及对凝血酶和胰蛋白酶的抑制常数 Ki 均有所降低.有趣的是,线性自由能关系(lfers)显示,与胰蛋白酶相比,Pka 值的降低对凝血酶的结合亲和力影响更大.在苯基氨定针的 F-替代对抑制剂三环骨架中的三级胺中心 Pka 值的影响上观测到了意外现象,随后通过 X 射线晶体学分析和从头计算进行了合理化.通过对小分子 X 射线晶体结构的分析和剑桥结构数据库(csd)的研究,获得了强方向性分子间 C-f⋯cn 交互作用的证据.
Doi:10.1039/b402515F

专利信息

专利号:US-9744252-B2
优先权日:2011-08-17
标 题:Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi
发明人：BERGER MARKUS; KRUGER MARTIN; LOHRKE JESSICA; REINHARDT MICHAEL; SIEBENEICHER HOLGER
权利人:PIRAMAL IMAGING SA
摘要:The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.

专利号:US-2008176865-A1
优先权日:2005-06-15
标 题:Substituted arylpyrazoles
发明人：BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
权利人:PFIZER LTD
摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

专利号:US-7645786-B2
优先权日:2005-06-15
标题:Substituted arylpyrazoles
发明人：BILLEN DENIS; BOYLE JESSICA; CRITCHER DOUGLAS JAMES; GETHIN DAVID MORRIS; HALL KIM THOMAS; KYNE GRAHAM MICHAEL
权利人:PFIZER
摘要:This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

专利号:CN-117924274-A
优先权日:2024-01-05
标 题:Synthesis method of non-neridrones