Development of PROTACs targeting estrogen receptor: An emerging technique for combating endocrine resistance DOI
Rouming Peng, Xin Liu, Chun‐Chi Chen

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 30, 2024

ER PROTACs emerge as a hopeful and innovative strategy for combating endocrine-resistant breast cancer.

Language: Английский

Efficient Stereoselective Synthesis of Vepdegestrant (ARV‐471) via Ruthenium‐Catalyzed Asymmetric Hydrogenation DOI
Neerasa Jayaprakash, Byeonggwan Kim, Hye Jin Chung

et al.

ChemistrySelect, Journal Year: 2025, Volume and Issue: 10(4)

Published: Jan. 1, 2025

Abstract Vepdegestrant (ARV‐471) is a novel estrogen receptor (ER) degrader currently under clinical evaluation for the treatment of ER‐positive and HER2‐negative breast cancer. We have developed an efficient catalytic stereoselective synthetic route to produce this important compound. The key step involves Ruthenium‐catalyzed asymmetric hydrogenation, which establishes critical stereocenter with exceptional diastereoselectivity(>99% de). This method obviates need chiral chromatographic separation, thereby significantly improving efficiency scalability sequence compared previously reported approaches.

Language: Английский

Citations

0
Development of PROTACs targeting estrogen receptor: An emerging technique for combating endocrine resistance DOI
Rouming Peng, Xin Liu, Chun‐Chi Chen

et al.

RSC Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 30, 2024

ER PROTACs emerge as a hopeful and innovative strategy for combating endocrine-resistant breast cancer.

Language: Английский

Citations

0