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Updated: Jul 14, 2026

One-pot Microwave-assisted Conversion of Anomeric Nitrate-esters to Trichloroacetimidates
Published on: January 15, 2018
Catalyst-free microwave-assisted amination of 2-chloro-5-nitrobenzoic acid
Younis Baqi1, Christa E Müller
1Pharmaceutical Chemistry I, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
Abstract:
The synthesis of N-substituted 5-nitroanthranilic acid derivatives 3a-w was achieved by a new, mild, microwave-assisted, regioselective amination reaction of 5-nitro-2-chlorobenzoic acid (1a) with a diverse range of aliphatic and aromatic amines 2a-w without added solvent or catalyst. Up to >99% isolated yield was obtained within 5-30 min at 80-120 degrees C. The reaction, which is suitable for upscaling, yielded new compounds that are of considerable interest as useful building blocks and as potential drugs.
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