A scalable and robust synthesis was developed for the preparation of a corticotropin releasing factor 1 (CRF1) receptor antagonist. Highlights of the strategy include formation of the hydroxytriazine core by a telescoped cyclization sequence and a novel catalyst-mediated chlorination reaction used to prepare the unstable penultimate species under mild conditions. Through many process improvements and efficient isolations of only 3 intermediates, the final product was obtained in high quality with an overall yield of 68%. 

Process development of a Corticotropin-Releasing Factor 1 (CRF1) receptor antagonist

240th National Meeting (2010)

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