期刊
CHEMICAL SCIENCE
卷 10, 期 2, 页码 569-575出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8sc04061c
关键词
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资金
- National Creative Research Initiative Grant through the National Research Foundation of Korea (NRF) - Korean Government (Ministry of Science and ICT) [NRF-2014R1A3A2030423]
- Bio & Medical Technology Development Program through the National Research Foundation of Korea (NRF) - Korean Government (Ministry of Science and ICT) [2012M3A9C4048780]
- BK21 Fellowship Program
Medium-sized heterocycles have recently received significant attention because of their potential roles as modulators of protein-protein interactions, but their molecular diversity and synthetic availability are still inadequate to meet the demand. To address these issues, we developed a new divergent synthetic pathway for skeletally distinct pyrimidine-containing medium-sized azacycles. We introduced N-quaternized pyrimidine-containing polyheterocycles as novel key intermediates for diversity-generating reactions via selective bond cleavages or migrations and prepared 14 discrete core skeletons in an efficient manner. The skeletal diversity of the resulting molecular frameworks was confirmed by chemoinformatic analysis.
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