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Showing 1–4 of 4 results
Advanced filters: Author: Filippo Romiti Clear advanced filters
  • Many bioactive compounds are trisubstituted macrocyclic alkenes, but use of current methods often results in poor yields and low stereoselectivity. Now, a ring-closing metathesis strategy has been developed that enables these compounds to be prepared efficiently and in either stereoisomeric form: an approach that may prove useful in the late stages of total syntheses, for skeletal editing and in drug discovery.

    • Yucheng Mu
    • Felix W. W. Hartrampf
    • Amir H. Hoveyda
    Research
    Nature Chemistry
    Volume: 14, P: 640-649
  • Orthogonal click reactions enable the rapid assembly of molecules of all sizes. Now, it has been shown that a nitrile, an allene, a diborane and a hydrazine or aniline can be catalytically merged in a click process that is orthogonal to SuFEx and CuAAC, delivering fluorescent linkages.

    • Paulo H. S. Paioti
    • Katherine E. Lounsbury
    • Amir H. Hoveyda
    Research
    Nature Chemistry
    Volume: 16, P: 426-436
  • Methods to access organofluorine compounds with a trifluoromethyl- and fluoro-substituted carbon stereogenic centre are severely limited. Now, a flexible and stereodivergent approach has been developed for the efficient preparation of homoallylic alcohols containing this moiety. Conversion to polyfluoro furanosides and pyranosides has been demonstrated, which is relevant to antiviral drug development.

    • Shibo Xu
    • Juan del Pozo
    • Amir H. Hoveyda
    Research
    Nature Chemistry
    Volume: 14, P: 1459-1469
  • Amines are commonly occurring units in many biologically active molecules. Now, a catalytic method has been developed that merges an unprotected/unactivated ketimine, a monosubstituted allene and a commercially available diboron reagent to afford versatile α-tertiary amines in up to 95% yield, >98% diastereomeric ratio and >99:1 enantiomeric ratio. The utility of this method was demonstrated through its application to the synthesis of the tricyclic core of a class of compounds with anti-Alzheimer activity.

    • Hwanjong Jang
    • Filippo Romiti
    • Amir H. Hoveyda
    Research
    Nature Chemistry
    Volume: 9, P: 1269-1275