Novartis Institutes for Biomedical Research , Horsham,West Sussex, RH12 5AB, United Kingdom.
J Am Chem Soc. 2014 Mar 19;136(11):4101-4. doi: 10.1021/ja412881j. Epub 2014 Mar 11.
A mild catalytic asymmetric direct fluoro-arylation of styrenes has been developed. The palladium-catalyzed three-component coupling of Selectfluor, a styrene and a boronic acid, provides chiral monofluorinated compounds in good yield and in high enantiomeric excess. A mechanism proceeding through a Pd(IV)-fluoride intermediate is proposed for the transformation and synthesis of an sp(3) C-F bond.
发展了一种温和的催化不对称直接芳基化反应。通过钯催化的 Selectfluor、苯乙烯和硼酸的三组分偶联,提供了手性单氟化化合物,产率高,对映选择性好。提出了一种通过 Pd(IV)-氟化物中间体进行转化和 sp(3) C-F 键合成的反应机制。