GDC-9545 is a selective estrogen receptor degrader (SERD) being developed by Genentech as a potential treatment for ER+/HER2- breast cancer. This talk will describe the development of a highly efficient and convergent route of GDC-9545. The design and development of a green and sustainable API manufacturing process featuring a high-throughput experimentation guided C–N coupling and crystallization-driven diastereoselective Pictet-Spengler reaction will be discussed in details.

Highly efficient asymmetric synthesis of selective estrogen receptor degrader GDC-9545

ACS Fall 2020 Virtual Meeting

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