801306-50-3Relevant academic research and scientific papers
First selective direct mono-arylation of piperidines using ruthenium-catalyzed C-H activation
Schwarz, Maria C.,Dastbaravardeh, Navid,Kirchner, Karl,Schnuerch, Michael,Mihovilovic, Marko D.
, p. 539 - 552 (2013/07/26)
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.
AMIDE DERIVATIVE
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Page/Page column 15-16, (2008/06/13)
An amide derivative represented by the formula (I) wherein A is a cycloalkyl group, an aryl group or a heteroaryl group, X is a nitrogen atom or CR17, Y is NRa, -(CRbRb')m- and the like, m is 0-4, and R1-R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having a substituent(s), ZR18 and the like, Z is -O-, -S(O)p-, -S(O)pO-, -NH-, -NR19- and the like, or R1 and R2 may in combination form a ring, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof is applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.
