Journal
SYNTHESIS-STUTTGART
Volume 52, Issue 17, Pages 2521-2527Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0040-1707400
Keywords
PROTACs; protein degradation; von Hippel-Lindau; VHL; E3 ligase; reductive amination; protecting group
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Funding
- Javna Agencija za Raziskovalno Dejavnost RS [Slovenian Research Agency (ARRS)] [P1-0208]
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The proteolysis-targeting chimeras (PROTACs) have become an integral part of different stages of drug discovery. This growing field, therefore, benefits from advancements in all segments of the design of these compounds. Herein, an efficient and optimized synthetic protocol to various von Hippel-Lindau (VHL) ligands is presented, which enables easy access to multigram quantities of these essential PROTAC building blocks. Moreover, the elaborated synthesis represents a straightforward approach to further explore the chemical space of VHL ligands.
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