The methyl group is one of the most commonly occurring carbon fragments in small‐
molecule drugs. This simplest alkyl fragment appears in more than 67% of the top‐selling …

The selective and efficient C–H methylation of sp2 and sp3 carbon centres has become a
powerful transformation in the synthetic toolbox. Due to the potential for profound changes to …

The “magic methyl” effect, a dramatic boost in the potency of biologically active compounds
from the incorporation of a single methyl group, provides a simple yet powerful strategy …

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 …

The so‐called magic methyl effect significantly boosts the bioactivities and physical
properties of pharmacologically active drugs. Direct introduction of the methyl group by C …

Methyl groups are well understood to play a critical role in pharmaceutical molecules,
especially those bearing saturated heterocyclic cores. Accordingly, methods that install …

The magic methyl effect is well acknowledged in medicinal chemistry, but despite its
significance, accessing such analogues via derivatization at a late stage remains a pivotal …

Over the past decade, the landscape of molecular synthesis has gained major impetus by
the introduction of late-stage functionalization (LSF) methodologies. C–H functionalization …

Site-selective C− H functionalization has emerged as an attractive tool for derivatizing
complex synthetic intermediates, but its use for late-stage diversification is limited by the …

The functionalization of carbon–hydrogen (C–H) bonds is one of the most attractive
strategies for molecular construction in organic chemistry. The hydrogen atom is considered …