Synthesis of Selective Estrogen Receptor Degrader GDC-0810 via Stereocontrolled Assembly of a Tetrasubstituted All-Carbon Olefin
收藏NIAID Data Ecosystem2026-03-10 收录
下载链接：
https://figshare.com/articles/dataset/Synthesis_of_Selective_Estrogen_Receptor_Degrader_GDC-0810_via_Stereocontrolled_Assembly_of_a_Tetrasubstituted_All-Carbon_Olefin/7111262
下载链接
链接失效反馈官方服务：
资源简介：
We report an efficient synthesis
of GDC-0810 on the basis of a
sequence involving a highly stereoselective lithium tert-butoxide-mediated enolization–tosylation (≥95:5 E:Z) and a Pd-catalyzed Suzuki–Miyaura
cross-coupling as key steps. Global deprotection, pyrrolidine salt
formation, and final active pharmaceutical ingredient (API) form control/isolation
produced GDC-0810 free acid in a 40% overall yield with >99.0%
purity
as ascertained by HPLC analysis.
创建时间：
2018-10-01
