📜甲基3-甲氧基-1,2-恶唑-5-羧酸酯置于sodium Hydroxide,水,盐酸体系中,用 N,N-二甲基甲酰胺,水 用作溶剂,化学反应 0.5H,反应生成3-甲氧基异恶唑-5-甲酸
参考文献:Practical Synthesis Of A Potent Bradykinin B1 Antagonist Via Enantioselective Hydrogenation Of A Pyridyl N-Acyl Enamide
标题:Practical Synthesis Of A Potent Bradykinin B1 Antagonist Via Enantioselective Hydrogenation Of A Pyridyl N-Acyl Enamide
摘要:A Practical And Efficient Synthesis Of Bradykinin B I Antagonist I Is Described. A Convergent Strategy Was Utilized Which Involved Synthesis Of Three Fragments: 3,6,And 7. Cross Coupling Of Fragments 6 And 7 Followed By Amidation With 3 Enabled Efficient Synthesis Of I In 19 Steps Total,A 35% Overall Yield From Commercially Available Pyridine 10. The Key To The Success Of The Synthesis Was The Development Of A Fluorodenitration Step To Install The Fluorine In Pyridine 7 And A Catalytic Enantioselective Hydrogenation Of N-Acyl Enamide 9 To Set The Stereochemistry.
Doi:10.1021/jo802772D