Wang Xisheng, Mei Tian-Sheng, Yu Jin-Quan
Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA.
J Am Chem Soc. 2009 Jun 10;131(22):7520-1. doi: 10.1021/ja901352k.
Pd(OTf)(2) x 2 H(2)O-catalyzed ortho-fluorination of triflamide-protected benzylamines is reported. The use of N-fluoro-2,4,6-trimethylpyridinium triflate as the F(+) source and NMP as a promoter is crucial for this reaction. The conversion of triflamide into a wide range of synthetically useful functional groups makes this fluorination protocol broadly applicable in medicinal chemistry and synthesis.
据报道，Pd(OTf)₂·2H₂O催化三氟甲酰胺保护的苄胺的邻位氟化反应。使用三氟甲磺酸N-氟-2,4,6-三甲基吡啶鎓作为氟源，N-甲基吡咯烷酮作为促进剂对该反应至关重要。三氟甲酰胺转化为多种具有合成用途的官能团使得这种氟化方法在药物化学和合成中具有广泛的适用性。
