HitGen has established a drug discovery research platform for small molecules and nucleic acid drugs centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies.
A highly efficient approach to C(sp3)−C(sp3) bond construction via on-DNA photoredox catalysis between on-DNA alkenes and N-aryl tertiary amines was developed. The methodology demonstrated 55%−95% conversions without obvious DNA damage, as seen by qPCR tests. Furthermore, various functional groups, such as carboxylic acids, aldehydes, and aryl halides, that can be used to create library diversities were shown to be tolerant of the C−H activation conditions.
Org. Lett., 2021, 23(9), 3486-3490
https://doi.org/10.1021/acs.orglett.1c00924
Link: https://pubs.acs.org/doi/10.1021/acs.orglett.1c00924
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