Benzenes, the most ubiquitous structural moiety in marketed small-molecule drugs, are
frequently associated with poor 'drug-like'properties, including metabolic instability, and poor …

Transition-metal-catalysed carbene insertion reaction is a straightforward and efficient
protocol for the construction of carbon–carbon or carbon–heteroatom bonds. Compared to …

Recent research in medicinal chemistry has suggested that there is a correlation between
an increase in the fraction of sp 3 carbons—those bonded to four other atoms—in drug …

The ortho-substituted phenyl ring is a basic structural element in chemistry. It is found in
more than three hundred drugs and agrochemicals. During the past decade, scientists have …

Strained bicyclic substructures are increasingly relevant in medicinal chemistry discovery
research because of their role as bioisosteres. Over the last decade, the successful use of …

Bicyclo [1.1. 1] pentane (BCP) motifs as para-disubstituted aryl bioisosteres are playing an
emerging role in pharmaceutical, agrochemical, and materials chemistry. The vast majority …

Abstract Bicyclic hydrocarbons, and bicyclo [1.1. 1] pentanes (BCPs) in particular, are
playing an emerging role as saturated bioisosteres in pharmaceutical, agrochemical and …

Modular functionalization enables versatile exploration of chemical space and has been
broadly applied in structure–activity relationship (SAR) studies of aromatic scaffolds during …

Catalytic borylations of sp 3 C–H bonds occur with high selectivities for primary C–H bonds
or secondary C–H bonds that are activated by nearby electron-withdrawing substituents …

Aryl amines are one of the most common moieties in biologically active molecules, and
approximately 37% of drug candidates contain aromatic amines. Recent advancements in …