GDC-0032 is an orally administrated potent PI3K kinase inhibitor discovered at Genentech and currently in PhI clinical trials for the treatment of cancer. In part II of this series, we will illustrate the various stages of the process development used to produce GDC-0032 on multikilogram scale. Multiple routes to the key starting materials were investigated, as well as a more efficient convergent end-game synthesis to the API. The optimized synthesis to the API will be highlighted in this talk.

Part II: Development of a manufacturing route to PI3K �-sparing inhibitor GDC-0032 (Taselisib)

248th National Meeting (2014)

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