Journal
ORGANIC LETTERS
Volume 23, Issue 3, Pages 908-913Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c04118
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Funding
- National Natural Science Foundation of China [21877117, 91953203, 21907103]
- National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China [2018ZX09711002-005]
- Personalized Medicines-Molecular Signature-based Drug Discovery and Development Strategic Priority Research Program of the Chinese Academy of Sciences [XDA12040330, XDA12050405]
- Shanghai Commission of Science and Technology [18431907100]
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By utilizing a diversity-oriented synthesis strategy with alpha,beta-unsaturated carbonyl compounds, DNA-compatible transformations for various heterocyclic scaffolds have been established, paving the way for preparing DNA-encoded libraries with more extensive chemical space.
Taking advantage of the diversity-oriented synthesis strategy with alpha,beta-unsaturated carbonyl compounds, we have successfully established the DNA-compatible transformations for various heterocyclic scaffolds. The ring-closure reactions for pyrrole, pyrrolidine, pyrazole, pyrazoline, isoxazoline, pyridine, piperidine, cyclohexenone, and 5,8-dihydroimidazo[1,2-a]pyrimidine were elegantly demonstrated in a DNA-compatible format. These efforts paved the way for preparing DNA-encoded libraries with more extensive chemical space.
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