期刊
ACS COMBINATORIAL SCIENCE
卷 18, 期 9, 页码 569-574出版社
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.6b00050
关键词
amino alcohols; fragment-based lead discovery; chiral fragments; drug discovery
资金
- NIGMS [GM038627]
- NSERC Canada
- Bayer Pharma AG
- Harvard University's Graduate Prize Fellowship
- HHMI Exceptional Research Opportunities Program (EXROP)
- Summer Research Opportunities at Harvard (SROH)
Efficient syntheses of chiral fragments derived from chiral amino alcohols are described. Several unique scaffolds were readily accessed in 1-5 synthetic steps leading to 45 chiral fragments, including oxazolidinones, morpholinones, lactams, and sultams. These fragments have molecular weights ranging from 100 to 255 Da and are soluble in water (0.085 to >15 mM).
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