ORGN 139 |
| 4-Halogeno-5-nitro anthranilic acid derivatives are important intermediates for a large variety of chemical products, however, reported synthetic method is based on a nitration at high temperature and safety issue related to the nitration is envisaged. We investigated an alternative synthesis of the anthranilic acid derivatives using amination via vicarious nucleophilic substitution with 1,1,1-trimethlhydrazinium iodide in the presence of t-BuOK. This reaction proceeded smoothly and the desired anthranilic acid was obtained by crystallization. Process safety examinations suggest that this method is suitable for large-scale manufacturing.
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Asymmetric Reactions and Syntheses, Physical Organic Chemistry, Combinatorial Chemistry, Total Synthesis
8:00 PM-10:00 PM, Sunday, 26 March 2006 Georgia World Congress Center -- Ex. Hall B4, Poster
Division of Organic Chemistry |
