The development of highly stereodefined synthesis to GDC-0810, a selective estrogen receptor degrader (SERD) via syn-elimination approach is described. This strategy is subsequently extended to a general methodology for stereoselective synthesis of tetrasubstituted acyclic all-carbon olefins through discovery of phosphate mediated, mild temperature syn-elimination. A systematic evaluation of diverse functional group tolerance will be discussed, along with a practical synthesis of tamoxifen using this chemistry.

Process development of GDC-0810 and the synthesis of highly stereodefined tetrasubstituted acyclic all-carbon olefins via a syn-elimination approach

256th National Meeting (2018)

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