参考标题:Synthesis Of A Muscarinic Receptor Antagonist Via A Diastereoselective Michael Reaction, Selective Deoxyfluorination And Aromatic Metal−halogen Exchange Reaction 作者:Toshiaki Mase,Ioannis N. Houpis,Atsushi Akao,Ilias Dorziotis,Khateeta Emerson,Thoa Hoang,Takehiko Iida,Takahiro Itoh,Keisuke Kamei,Shinji Kato,Yoshiaki Kato,Masashi Kawasaki,Fengrui Lang,Jaemoon Lee,Joseph Lynch,Peter Maligres,Audrey Molina,Takayuki Nemoto,Shigemitsu Okada,Robert Reamer,Jake Z. Song,David Tschaen,Toshihiro Wada,Daniel Zewge,R. P. Volante,Paul J. Reider,Koji Tomimoto |发布日期:2001.10.1 摘要:6-Bromo-2-Formylpyridine (26) In Excellent Yield. Further Transformations Afforded The Amine Fragment 3 Via Reductive Amination With 35, Pd-Catalyzed Aromatic Amination, And Deprotection. Finally, The Highly Convergent Synthesis Of 1 Was Accomplished By Coupling Of The Two Fragments. This Synthesis Has Been Used To Prepare Multi-Kilogram Quantities Of The Bulk Drug.