CAS: 406233-26-9; 4-(4,4-Dimethylpiperidin-1-yl)Benzoic Acid

上下游产品

CAS号406233-25-8 4-(4,4-二甲基哌啶子基)苯甲酸乙酯 | CAS号279692-23-8 4-(4,4-二甲基-2,6-... | CAS号4160-82-1 3,3-二甲基戊二酸酐 | CAS号94-09-7 对氨基苯甲酸乙酯

📜2,2,2,4'-四氟苯乙酮置于三乙胺,Sodium Hydroxide体系中,用 水,二甲基亚砜,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 18.0H,反应生成 4-(4,4-二甲基哌啶-1-基)苯甲酸
参考文献:Molecular Dynamics Study-Guided Identification Of Cyclic Amine Structures As Novel Hydrophobic Tail Components Of Hpparγ Agonists
标题:Molecular Dynamics Study-Guided Identification Of Cyclic Amine Structures As Novel Hydrophobic Tail Components Of Hpparγ Agonists
摘要:We Previously Reported That A α-Benzylphenylpropanoic Acid-Type Hpparγ-Selective Agonist With A Piperidine Ring As The Hydrophobic Tail Part (3) Exhibited Sub-Micromolar-Order Hpparγ Agonistic Activity. In Order To Enhance The Activity,We Planned To Carry Out Structural Development Based On Information Obtained From The X-Ray Crystal Structure Of Hpparγ Ligand Binding Domain (Lbd) Complexed With 3. However,The Shape And/or Nature Of The Binding Pocket Surrounding The Piperidine Ring Of 3 Could Not Be Precisely Delineated Because The Structure Of The Omega Loop Of The Lbd Was Poorly Defined. Therefore,We Constructed And Inserted A Plausible Omega Loop By Means Of Molecular Dynamics Simulation. We Then Used The Reconstructed Lbd Structure To Design New Mono-,Bi-And Tricyclic Amine-Bearing Compounds That Might Be Expected To Show Greater Binding Affinity For The Lbd. Here,We Describe Synthesis And Evaluation Of α-Benzylphenylpropanoic Acid Derivatives 8. As Expected,Most Of The Newly Synthesized Compounds Exhibited More Potent Hpparγ Agonistic Activity And Greater Hpparγ Binding Affinity Than 3. Some Of These Compounds Also Showed Comparable Aqueous Solubility To 3.
DOI:10.1016/j.Bmcl.2014.06.023

专利信息

专利号:US-2013203709-A1
优先权日:2010-08-09
标 题 :Acylsulfonamides and processes for producing the same
发明人：MANETSCH ROMAN; KULKARNI SAMEER; IYAMU IREDIA D; WANG HONG-GANG; DOI KENICHIRO; GUIDA WAYNE; SANTIAGO DANIEL; DU BOULAY COURTNEY
权利人:MANETSCH ROMAN; KULKARNI SAMEER; IYAMU IREDIA D; WANG HONG-GANG; DOI KENICHIRO; GUIDA WAYNE; SANTIAGO DANIEL; DU BOULAY COURTNEY; PENN STATE RES FOUND; UNIV SOUTH FLORIDA
摘要:The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.

专利号:US-8524947-B2
优先权日:2008-02-22
标题 :Acylsulfonamides and processes for producing the same
发明人：WANG HONG-GANG; MANETSCH ROMAN; HU XIANGDONG; KULKARNI SAMEER; SUN JIAZHI
权利人:WANG HONG-GANG; MANETSCH ROMAN; HU XIANGDONG; KULKARNI SAMEER; SUN JIAZHI; UNIV SOUTH FLORIDA; H LEE MOFFITT CANCER CT & RES
摘要:The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.