Synthesis of Benzothiazinones from Benzoyl Thiocarbamates: Application to Clinical Candidates for Tuberculosis Treatment

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Benzothiazinones are a structural motif found in biologically active compounds, such as the clinical candidates BTZ‐043 and Macozinone for the treatment of tuberculosis. We describe a robust, two‐step method to synthesize 2‐amino‐substituted benzothiazinones from benzoyl thiocarbamates, which were prepared in a one‐pot procedure from benzoyl chlorides. The intramolecular cyclization and ethoxy displacement steps were also amenable to adoption in continuous flow as exemplified by select substrates.