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Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments

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2016

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American Chemical Society
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Haftchenary, S., S. D. Nelson, L. Furst, S. Dandapani, S. J. Ferrara, Ž. V. Bošković, S. Figueroa Lazú, et al. 2016. “Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments.” ACS Combinatorial Science 18 (9): 569-574. doi:10.1021/acscombsci.6b00050. http://dx.doi.org/10.1021/acscombsci.6b00050.

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Abstract

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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amino alcohols, fragment-based lead discovery, chiral fragments, drug discovery

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