Oxidation is the main pathway of drug metabolism and cytochrome P-450 (CYP450)
enzymes account for over 80% of drug oxidation. The chemical outcome of this first-pass …

Developing approaches to predictably selective functionalization of aliphatic C–H bonds has
long been one of the major challenges (“Holy grails”, Bergman, Acc. Chem. Res. 28 (1995) …

Compared with the extensively reported hydrogen atom transfer (HAT) at sp3 C–H,
abstraction of hydrogen atoms at the sp2 carbon is extremely rare. Here, we communicate …

Postsynthetic diversification of peptides through selective modification of endogenous amino
acid side chains has enabled significant advances in peptide drug discovery while …

Abstract α-Ketoglutarate dependent nonheme halogenases catalyze regioselective
functionalization of aliphatic Csingle bondH bonds via H abstraction by the ferryl site of the …

Under mild blue-light irradiation, α-acylated saturated heterocycles undergo a
photomediated one-atom ring contraction that extrudes a heteroatom from the cyclic core …

Unnatural amino acids, and their synthesis by the late‐stage functionalization (LSF) of
peptides, play a crucial role in areas such as drug design and discovery. Historically, the …

We disclose a benzylic C–H oxidative coupling reaction with alcohols that proceeds through
a synergistic deprotonation, halogenation and substitution sequence. The combination of …

This review analyses the chemical characteristics of arylhydrazonals in depth, with a
particular emphasis on their critical function in heterocyclic synthesis. Arylhydrazonals are …

The transition metal-free Cs2CO3/Oxone®-mediated C3-alkylation of indoles proceeds in
moderate to high yields with a variety of C4–C7 functionalized indoles and is applicable to 2 …