Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, United States.
Org Lett. 2010 Nov 19;12(22):5112-5. doi: 10.1021/ol102246d. Epub 2010 Oct 20.
Spirooxindole amides can be prepared by the intramolecular addition of functionalized indoles into acylimines that are accessed from nitriles by hydrozirconation and acylation. The stereochemical outcome at the quaternary center was controlled by the steric bulk of the substituent at the 2-position of the indole unit. The products are well-suited for diversification to prepare libraries.
螺环氧化吲哚酰胺可以通过官能化吲哚与酰亚胺的分子内环加成来制备,酰亚胺可通过氰基的氢化锆和酰化作用得到。在季碳原子处的立体化学产物可以通过吲哚单元 2 位取代基的空间位阻来控制。这些产物非常适合进行多样化衍生以制备文库。