Late-stage oxidative C(sp3)–H methylation Frequently referred to as the 'magic methyl effect', the installation of methyl groups—especially adjacent (α) to heteroatoms—has been shown to dramatically increase the potency of biologically active molecules. However, existing meth... Kaibo Feng,Raun...
Nitrogen heterocycle represents a ubiquitous skeleton in natural products and drugs. Late-stage C(sp3)-H bond functionalization of N-heterocycles with broad substrate scope remains a challenge and of particular significance to modern chemical synthesis a
stage functionalizations were included in the training data such as P450 catalyzed oxidations (642 reactions), electrochemical methylations (12 reactions), and photoredox alkylations (93 reactions) (see TableS2for further breakdown of the dataset). Reactions that yielded oxidative cleavage or hydrolyzed...
Merging two functions in a single Rh catalyst system: bimodular conjugate for light-induced oxidative coupling J. Am. Chem. Soc., 142 (2020), pp. 19052-19057 Google Scholar 13 S.D. Friis, M.J. Johansson, L. Ackermann Cobalt-catalysed C–H methylation for late-stage drug diversification ...
Peptides and peptidomimetics are emerging as an important class of clinic therapeutics. Here we report a peptide-guided method for the functionalization and macrocyclization of bioactive peptidosulfonamides by Pd(II)-catalyzed late-stage C–H activation.