The development of a robust synthesis of a CRTH2/DP antagonist AMG 853 is presented. The key step in the synthesis is a Pd-catalyzed sulfonamide coupling. A mechanistic study of the cross-coupling reaction established a link between catalyst deactivation and impurity formation. This presentation will describe how control of drug substance purity was established by process understanding.

Development and investigation of a Pd-catalyzed C-N bond formation: Application to the synthesis of an active pharmaceutical ingredient

253rd National Meeting (2017)

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