The expansion of the chemical space to tangible libraries containing billions of
synthesizable molecules opens exciting opportunities for drug discovery, but also …

The methoxy substituent is prevalent in natural products and, consequently, is present in
many natural product-derived drugs. It has also been installed in modern drug molecules …

The development of bimolecular homolytic substitution (SH2) catalysis has expanded cross-
coupling chemistries by enabling the selective combination of any primary radical with any …

The first oxidative chloro-and bromodifluoromethylation of phenols with (CH3) 3SiCF2X and
CuX (X= Cl or Br) in the presence of Selectfluor under mild reaction conditions was …

Carboxylates are ideal directing groups because they are widely available, readily
cleavable and excellent linchpins for diverse follow-up reactions. However, their use in meta …

Halogenation is one of the most important transformations in organic synthesis.
Halogenated compounds are employed in many reactions to prepare useful molecules …

Purpose Over the last few years, covalent fragment-based drug discovery has gained
significant importance. Thus, striving for more warhead diversity, we conceived a library …

Organofluorine compounds have greatly benefited the pharmaceutical, agrochemical, and
materials sectors. However, they are plagued by concerns associated with Per-and …

Here, we describe a novel strategy for chemoselective synthesis of α-halo-α, α-
difluoromethyl ketones (− COCF3 and− COClCF2 motifs) from trimethyl (phenylethynyl) …

Due to their versatile properties, phenolic compounds are integral to various biologically
active molecules, including many pharmaceuticals. However, their application in drug …