📜3-溴苯磺酰氯,异丙胺 以 四氢呋喃 作为反应溶剂,化学反应 0.5H,反应生成 N-异丙基-3-溴苯磺酰胺
参考文献:Synthesis And Structure−activity Relationships Of Long-Acting β2 Adrenergic Receptor Agonists Incorporating Arylsulfonamide Groups
标题:Synthesis And Structure−activity Relationships Of Long-Acting β2 Adrenergic Receptor Agonists Incorporating Arylsulfonamide Groups
摘要:A Series Of Saligenin Alkoxyalkylphenylsulfonamide Beta(2) Adrenoceptor Agonists Were Prepared By Reacting A Protected Saligenin Oxazolidinone With Alkynyloxyalkyl Bromides,Followed By Sonogashira Reaction,Hydrogenation,And Deprotection. The Meta-Substituted Primary Sulfonamide Was More Potent Than The Para And The Ortho-Analogues. Primary Sulfonamides Were More Potent Than The Secondary And Tertiary Analogues. The Onset And Duration Of Action In Vitro Of Selected Compounds Was Assessed On Isolated Superfused Guinea Pig Trachea. Sulfonamide 29B Had The Best Profile Of Potency,Selectivity,Onset,And Duration Of Action On Both Guinea Pig Trachea And Human Bronchus. Furthermore,29B Was Found To Have Low Oral Bioavailability In Rat And Dog And Also To Have Long Duration Of Action In An In Vivo Model Of Bronchodilation. Crystalline Salts Of 29B Were Identified That Had Suitable Properties For Inhaled Administration. A Proposed Binding Mode For 29B To The Beta(2)-Receptor Is Presented.
DOI:10.1021/jm801016J