Journal
ACS OMEGA
Volume 7, Issue 30, Pages -Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.2c00245
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Funding
- Arkansas Research Alliance
- NIH [R01CA248037, R01CA256158, R01]
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This paper reports a column chromatography-free process for the rapid synthesis of VH032 amine hydrochloride, a key building block for VHL E3 ligase-based PROTACs. The process enables the production of VH032 amine hydrochloride in high yield and purity, providing an important method for the construction of VHL PROTAC libraries.
PROTACs represent a promising modality that has gained significant attention for the treatment of cancer, Alzheimer's disease, and so forth. Due to limited structural information of the POI-PROTAC-E3 ligase ternary complex, the discovery of active PROTACs relies on the screening of diversity-oriented PROTAC libraries. VH032 amine is a key building block for the synthesis of VHL E3 ligase-based PROTACs. To construct VHL PROTAC libraries rapidly, the availability of VH032 amine is crucial. In this paper, we report a column chromatography-free process which enables the production of 42.5 g of VH032 amine hydrochloride in 65% overall yield with 97% purity in a week.
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