CAS: 208111-00-6; 6-(Thiophen-2-yl)Picolinaldehyde

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3319-99-1 501378-56-9 887981-86-4

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CAS号33674-97-4 2-氯-6-羟甲基吡啶

📜6-氯-2-羟甲基吡啶置于镍 盐酸,六甲基磷酰三胺,4-二甲氨基吡啶,Manganese(Iv) Oxide,四(三苯基膦)钯,Ti2Co3,4 A Molecular Sieve,氢气,Sodium Hydride,N,N-二异丙基乙胺体系中,用 四氢呋喃,吡啶,乙醇,二氯甲烷,苯 用作溶剂,化学反应 58.0H,反应生成6-(2-噻吩基)-2-吡啶醛
参考文献:Design And Synthesis Of A Series Of 6-Substituted-2-Pyridinylmethylamine Derivatives As Novel,High-Affinity,Selective Agonists At 5-Ht1A Receptors
标题:Design And Synthesis Of A Series Of 6-Substituted-2-Pyridinylmethylamine Derivatives As Novel,High-Affinity,Selective Agonists At 5-Ht1A Receptors
摘要:A Search For Novel,Selective Agonists With High Intrinsic Activity At The 5-Ht1A Subtype Of Serotonin (5-Ht) Receptors Was Undertaken. Mechanistic And Thermodynamic Considerations Led To The Design Of 6-Substituted-2-Pyridinylmethylamine As A Potential 5-Ht1A Pharmacophore. Various Adducts Derived From The 6-Substituted-2-Pyridinylmethylamine Moiety Were Tested For Their Affinity At 5-Ht1A,Alpha(1)-Adrenergic,And D-2-Dopaminergic Receptors. Compounds With High Affinity For 5-Ht1A Receptors (Pk(I) Greater Than Or Equal To 8) Were Examined For Agonist Properties By Measuring Their Ability To Inhibit Forskolin-Stimulated Camp Production In Ha7 Cells (I.E.,Hela Cells Permanently Transfected With The H5-Ht1A Receptor Gene And Expressing The H5-Ht1A Receptor Protein). Several Compounds Of The Type Aryl{4-[(6-Substituted-Pyridin-2-Ylmethylamino)Methyl]Piperidin-1-Yl}Methanone Had Nanomolar Affinity For 5-Ht1A Binding Sites And Were More Than 500-Fold Selective With Respect To Alpha(1) And D-2 Sites. Importantly,Their 5-Ht1A Agonist Properties Were Demonstrated In Ha7 Cells Where They Behaved As Potent Inhibitors Of Camp Accumulation. In Particular,(3,4-Dichlorophenyl){4-[(6-Oxazol-5-Ylpyridin-2-Ylmethylamino)Methyl]Piperidin-1-Yl}Methanone (70) And (3,4-Dichlorophenyl){4-[(6-Azetidinopyridin-2-Ylmethylamino)Methyl]Piperidin-1-Yl}Methanone (36) Appeared To Be More Potent Than,And At Least As Efficacious As,The Prototypical 5-Ht1A Agonist (+/-)-8-Oh-Dpat. Sar Studies Revealed That The Pyridine Nitrogen Atom And The Nature And The Position Of The Substituents On The Pyridine Ring Were Critically Involved In The Ability Of The Compounds To Recognize And Activate 5-Ht1A Receptors. Structural Modifications Of The Nonpharmacophoric Part Of The Molecule Showed,However,That The Entire Structure Was Required For Affinity At 5-Ht1A Binding Sites.
Doi:10.1021/jm9804329