This Perspective is a continuation of our analysis of US FDA-approved small-molecule drugs
(1938–2012) containing nitrogen heterocycles. In this study we report drug structure and …

Inspired by the success of fluorinated corticosteroids in the 1950s and fluoroquinolones in
the 1980s, fluorine-containing pharmaceuticals, which are also known as fluoro …

In the present work, we report compilation and analysis of 245 drugs, including small and
macromolecules approved by the US FDA from 2015 until June 2020. Nearly 29% of the …

(Hetero) aromatic compounds are vastly available and easy to functionalise building blocks
in the chemical industry. Asymmetric arene hydrogenation enables direct access to complex …

N-heterocycles are important, not only because of their abundance, but above all because of
their chemical, biological and technical significance. They play an important role in …

Abstract C (sp 3)-rich bicyclic hydrocarbon scaffolds, as exemplified by bicyclo [1.1. 1]
pentanes, play an increasingly high-profile role as saturated bioisosteres of benzenoids in …

Caffeic acid (CA) is found abundantly in fruits, vegetables, tea, coffee, oils, and more. CA
and its derivatives have been used for many centuries due to their natural healing and …

Phenols and phenolic ethers are significant scaffolds recurring both in nature and among
approved small-molecule pharmaceuticals. This compendium presents the first …

Abstract Design, synthesis and application of benzene bioisosteres have attracted a lot of
attention in the past 20 years. Recently, bicyclo [2.1. 1] hexanes have emerged as highly …

Synthesis of bicyclic scaffolds has gained significant attention in drug discovery due to their
potential to mimic benzene bioisosteres. Here, we present a mild and scalable Sc (OTf) 3 …