Triflic acid-catalyzed Csp3-H functionalization of 2-methyl azaarenes with a α-trifluoromethyl imino ester

A Brønsted acid promoted Csp3-H functionalization of 2-alkyl azaarenes with α-trifluoromethylated imino ester is described. A catalytic amount of triflic acid provided straightforward access to the corresponding trifluoromethylated amino esters via concomitant in situ one step N-alkyl deprotection. On further hydrolysis of ester, synthesis of quinoline derived unnatural trifluoromethylated amino acids has been achieved in a short and efficient manner.