Schwarz Maria C, Dastbaravardeh Navid, Kirchner Karl, Schnürch Michael, Mihovilovic Marko D
Institute of Applied Synthetic Chemistry, Vienna University of Technology, Getreidemarkt 9/163-OC, 1060 Vienna, Austria.
Monatsh Chem. 2013;144(4):539-552. doi: 10.1007/s00706-013-0947-1. Epub 2013 Apr 3.
A Ru-catalyzed mono-arylation in α-position of saturated cyclic amines is reported employing a C-H activation protocol. Substitution of the pyridine directing group with a bulky group, e.g., trifluoromethyl in the 3-position, proved to be crucial to avoid bis-arylation. This highly selective transformation can be performed with different amines and arylboronate esters. Additionally, the directing group can be cleaved, taking advantage of an unprecedented detrifluoromethylation reaction.
报道了一种采用C-H活化方案在饱和环胺α位进行的钌催化单芳基化反应。事实证明，用大体积基团（如3位的三氟甲基）取代吡啶导向基团对于避免双芳基化至关重要。这种高度选择性的转化反应可以用不同的胺和芳基硼酸酯来进行。此外，利用一种前所未有的脱三氟甲基化反应，可以裂解导向基团。
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