The development of methylation protocol has attracted intense attention owing to"magic methyl effect"in drug discovery.Meanwhile,the indole scaffold is prevalence in the natural products and pharmacophores.D...The development of methylation protocol has attracted intense attention owing to"magic methyl effect"in drug discovery.Meanwhile,the indole scaffold is prevalence in the natural products and pharmacophores.Despite the advances in other site selective methylation,there is scarce reports for C4 methylation of indoles and combination of a carbonyl group rearrangement with C—H methylation on indole ring.Herein,the C4 methylation of indoles and the steric controlled C4-methylation/carbonyl group migration are reported.The large steric hindrance at carbonyl group facilitates the carbonyl group migration,which provides a straightforward protocol for the synthesis of C2/C4 disubstituted indoles.展开更多
基金Project supported by the University Nursing Program for Young Scholars with Creative Talents in Heilongjiang Province(No.UNPYSCT-2017124)。
文摘The development of methylation protocol has attracted intense attention owing to"magic methyl effect"in drug discovery.Meanwhile,the indole scaffold is prevalence in the natural products and pharmacophores.Despite the advances in other site selective methylation,there is scarce reports for C4 methylation of indoles and combination of a carbonyl group rearrangement with C—H methylation on indole ring.Herein,the C4 methylation of indoles and the steric controlled C4-methylation/carbonyl group migration are reported.The large steric hindrance at carbonyl group facilitates the carbonyl group migration,which provides a straightforward protocol for the synthesis of C2/C4 disubstituted indoles.
