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Updated: Sep 30, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
Bismuth-catalyzed arylation of ethyl glyoxylate with aniline via N-H insertion
Mohd Aamir Bin Riyaz1, G Premkumar1, Toka Swu2
1Department of Chemistry, Pondicherry University, R.V. Nagar, Kalapet, Puducherry, 605014, India.
Abstract:
Glycine derivatives such as ethyl 2-(4-aminophenyl)-2-(phenylamino) acetate is an exciting and essential non-proteinogenic class of amino acids. Herein, we report an efficient and novel route to synthesize glycine derivatives using ethyl glyoxylate, aniline, and its derivatives catalyzed by bismuth salts. In our scheme, mild, non-toxic, and commercially viable reagents were utilized. The synthesized moieties were characterized by ESI-MASS, 1H-NMR, 13C-NMR, and XRD techniques. The target glycine derivatives were successfully obtained with a maximum yield of 87%. Moreover, the reaction is very green as water is the only byproduct.
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