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Synthesis 2020; 52(17): 2521-2527
DOI: 10.1055/s-0040-1707400
DOI: 10.1055/s-0040-1707400
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A Facile Synthesis of Ligands for the von Hippel–Lindau E3 Ligase
I.S. acknowledges funding by the Javna Agencija za Raziskovalno Dejavnost RS [Slovenian Research Agency (ARRS)] through research core funding No. P1-0208.Weitere Informationen
Publikationsverlauf
Received: 05. März 2020
Accepted after revision: 06. Mai 2020
Publikationsdatum:
27. Mai 2020 (online)
Abstract
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.
Key words
PROTACs - protein degradation - von Hippel–Lindau - VHL - E3 ligase - reductive amination - protecting groupSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0040-1707400.
- Supporting Information
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