The amide functional group plays a key role in the composition of biomolecules, including
many clinically approved drugs. Bioisosterism is widely employed in the rational …

The electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …

C–F bond activation has drawn a lot of attention in the past, and the case of C (sp3)–F bonds
is particularly interesting as those are the strongest single bonds carbon makes with any …

Monofluoroalkenes have found wide application in organic chemistry, medicinal chemistry,
and materials science. This review summarizes the most recent advances made regarding …

Introduction There continues to be an exponential rise in the number of small molecule
drugs that contain either a fluorine atom or a fluorinated fragment. While the unique …

Isosteric replacement of amide groups is a classic practice in medicinal chemistry. This
digest highlights the applications of most commonly employed amide isosteres in drug …

Abstract gem‐Heteroatom‐substituted fluoroalkenes have received little attention despite
their great potential in medicinal chemistry or in fine chemistry. Indeed, due to the electronic …

A Pd-catalyzed ring-opening sulfonylation of gem-difluorocyclopropanes is reported. This
protocol involves C–C bond cleavage, β-F elimination, and allylic coupling to form …

Despite various advantages, opioid peptides have been limited in their therapeutic uses due
to the main drawbacks in metabolic stability, blood-brain barrier permeability, and …

Monofluoroalkenes are fluorinated motifs that can be used to replace amide bonds. In order
to be incorporated into peptides, it is normally necessary to first synthesize a dipeptide …