First selective direct mono-arylation of piperidines using ruthenium-catalyzed C–H activation

…, N Dastbaravardeh, K Kirchner, M Schnürch…

Index: Schwarz, Maria C.; Dastbaravardeh, Navid; Kirchner, Karl; Schnuerch, Michael; Mihovilovic, Marko D. Monatshefte fur Chemie, 2013 , vol. 144, # 4 p. 539 - 552

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Citation Number: 8

Abstract

Abstract 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, eg, 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 ...