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    Enantio‐ and Diastereoselective Cyclopropanation of 1‐Alkenylboronates : Synthesis of 1‐Boryl‐2,3‐Disubstituted Cyclopropanes

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    A novel, highly enantio- and diastereoselective synthesis of 1-boryl-2,3-disubstituted cyclopropanes has been developed by means of the cyclopropanation of alkenylboronates with ethyl diazoacetate in the presence of catalytic amounts of a chiral copper(I) complex. The products can also be directly accessed from alkynes through an operationally simple, sequential hydroboration–cyclopropanation protocol. The resulting enantioenriched 1-boryl-2,3-disubstituted cyclopropanes are versatile synthetic intermediates that undergo further transformations at the carbon–boron bond.We thank MINECO for financial support (CTQ2014-52769- C03-01-R and Juan de la Cierva fellow for J.C.) and Junta de Andaluc a (P12-FQM-1765). We also thank Riccardo Gava and Cristina Gonzalez for additional experiments and Francisco Molina for X-ray diffraction studies
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