Solution-phase parallel synthesis of highly diverse spiroisoxazolinohydantoins |
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Authors: | Hao-Wei Shih |
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Affiliation: | The Genomics Research Center, Academia Sinica, No. 128, Academia Road, Section 2, Nankang District, Taipei 11529, Taiwan |
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Abstract: | Practical and efficient solution-phase parallel synthesis of spiroisoxazolinohydantoins under mild conditions has been developed. This spiroisoxazolinohydantoin skeleton possesses three diversity points. The key intermediate, exo-methylenehydantoin bearing two positions of diversification, is prepared via a one-pot synthetic route from N-substituted methyl ester serine. Employing various alkyl halides, isocyanates, and oximes, this chemistry is applied in the generation of an 18-member demonstration library with high yield, high purity and excellent regioselectivity. |
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Keywords: | Spiro compounds Solution-phase combinatorial chemistry Isoxazoline Hydantoin |
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