胺气处理
组合化学
重新使用
化学
计算机科学
工程类
有机化学
废物管理
作者
Wei Yan,Bo Pan,Jingwei Shao,Hui Lin,Hongyu Li
出处
期刊:ACS omega
[American Chemical Society]
日期:2022-07-19
卷期号:7 (30): 26015-26021
被引量:4
标识
DOI:10.1021/acsomega.2c00245
摘要
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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