Asymmetric synthesis of orthogonally protected trans-cyclopropane c-amino acids via intramolecular ring closure

Date

2006

Authors

Fox, David J.
Pedersen, Daniel Sejer
Warren, Stuart

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Journal article

Citation

Organic and Biomolecular Chemistry, 2006; 4(16):3113-3116

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David J. Fox, Daniel Sejer Pedersen and Stuart Warren

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Abstract

The synthesis of enantiomerically-enriched trans-cyclopropane amino- and hydroxy-acids can be achieved by intramolecular ring closure in moderate to good yields. The optically active cyclopropane precursors are easily prepared in a short sequence from inexpensive, commercially available olefins and tert-butyl acetate. Several leaving groups and bases were compared for the cyclopropanation step, showing that the diphenylphosphinate and tosyl leaving groups give the best results when used in combination with either LDA or NaHMDS.

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School of Chemistry and Physics : Chemistry

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© The Royal Society of Chemistry 2006

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