Laboratorium für Organische Chemie, Department of Chemistry and Applied Biosciences , ETH Zürich , 8093 Zürich , Switzerland.
Org Lett. 2018 Apr 20;20(8):2378-2381. doi: 10.1021/acs.orglett.8b00720. Epub 2018 Apr 5.
A one-step synthesis of aliphatic KATs from organocuprates is reported. Organolithium and organomagnesium reagents were readily transmetalated onto Cu(I) and coupled with a KAT-forming reagent to yield the respective aliphatic KAT. The protocol is suitable for primary, secondary and-for the first time-tertiary alkyl substrates. These protocols considerably expand the range of KATs that can be readily accessed in one step from commercially available starting materials.
报道了一种从有机铜试剂一步合成脂肪族 KAT 的方法。有机锂和有机镁试剂容易与 Cu(I)发生转金属化反应，并与 KAT 形成试剂偶联，得到相应的脂肪族 KAT。该方案适用于伯、仲烷基底物，并且首次适用于叔烷基底物。这些方案大大扩展了可从商业上可获得的起始原料一步容易获得的 KAT 的范围。
