AZD9977 is a neutral and selective MR modulator in clinical development for heart failure. During our work to identify backups, we expanded the SAR to include a range of sulfonamide derivatives as represented by compound 1, which showed excellent binding to hMR. However, the preparation of these sulfonamide analogs posed a significant challenge to the synthetic chemists. Herein we report on the preparation of these sulfonamide analogs and in detail the route development of 1, which led to a relatively short scalable chemistry route on a 100-gram scale to support preclinical profiling before CD nomination.

Route development of synthetically challenging sulfonamide analogs of the MR modulator AZD9977

256th National Meeting (2018)

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