Efficient Stereoselective Synthesis of Vepdegestrant (ARV‐471) via Ruthenium‐Catalyzed Asymmetric Hydrogenation

ChemistrySelect, Год журнала: 2025, Номер 10(4)

Опубликована: Янв. 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.

Язык: Английский

Design, Synthesis, and Biological Evaluation of Novel BTK-targeting Proteolysis Targeting Chimeras (PROTACs) with Enhanced Pharmacokinetic Properties

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер 289, С. 117420 - 117420

Опубликована: Фев. 22, 2025

Язык: Английский

Development of PROTACs targeting estrogen receptor: An emerging technique for combating endocrine resistance

RSC Medicinal Chemistry, Год журнала: 2024, Номер unknown

Опубликована: Дек. 30, 2024

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

Язык: Английский