James Bull

Bioisosteres represent a powerful tool for medicinal chemists to modulate and improve structural and pharmacokinetic properties of bioactive compounds in the development of pharmaceuticals. Benzamides are an important pharmacophore which is present in over 100 approved drugs…

A handful of robust and reliable reactions have a disproportionate influence on the medicinal chemist’s toolbox to construct molecules and investigate chemical space. Importantly, click reactions have emerged as a class of reactions that proceed on a very broad scope under mild conditions…

Annulation reactions provide an important and divergent approach to desirable ring systems by combining two fragments containing appropriate functionalities. Usually, these link matched nucleophilic and electrophilic sites on each component (e.g…

3,3-Disubstituted oxetanes have garnered considerable interest as isosteres of carbonyl groups and as new design elements for medicinal chemists. Despite their popularity, methods to access 3,3-disubstituted oxetanes are scarce, particularly for 3,3-dicarbon substitutions…

As modern drug design moves away from sp2-rich molecules toward more 3D space, novel substitutions at benzylic positions offer the vectors for novel conformational designs to pharmaceutically relevant molecules…

Sulfonamides are used extensively in the agrochemical and medicinal chemistry industries. However, until recently the use of their aza-analogues, sulfoximines and sulfonimidamides, has been limited…

Photoredox catalyzed C(sp3)–H functionalization is a powerful technique to access derivatized heterocycles under mild conditions with wide functional group tolerance…

Energetic functional groups offer powerful reactivity, but interest in their synthetic possibilities is usually tempered by concerns over instability or explosive behaviour…

Oxetanes and azetidines are increasingly valued in drug discovery due to favourable lipophilicity, molecular weight and scaffolding properties. Oxetanes in particular offer intriguing potential as carbonyl replacement groups…

F-gases are commonly used as refrigerants, aerosols and blowing agents, but can have serious environmental impact when released into the atmosphere…

Oxetanes and azetidines are increasingly common in drug discovery campaigns and in clinical candidate compounds. 3,3-Disubstituted oxetanes in particular have been demonstrated to provide attractive physicochemical properties and offer potential mimics of carbonyl derivatives in new chemical space…

Spirocyclic compounds have emerged as attractive scaffolds in medicinal chemistry. Their increased conformational rigidity and three-dimensionality provide well defined exit vectors to enhance ligand binding interactions…

As drug discovery campaigns continue to target evermore challenging biological targets, there is an increasing demand for drug candidates to possess greater molecular complexity…

Stereocontrolled synthesis of chiral molecules is essential in ensuring positive three-dimensional interactions with biological targets. Achiral sulfur(VI) motifs, such as sulfonamides and sulfones, are prevalent across medicinal and agricultural chemistry…

The development of novel chemical motifs and building blocks is essential to enable the rapid generation of molecular complexity and the exploration of new chemical space. Fluorinated cycloalkyl building blocks have garnered particular attention, including the _gem_-difluorocyclobutane moiety…

There is an ongoing search for new, validated design options that can modulate binding and physiochemical properties of a compound…

Sulfur-containing functional groups at different oxidation states are important motifs in medicinal chemistry and often found in bioactive natural products…

Synthetic electrochemistry has gained renewed attention as a sustainable and viable platform for organic synthesis…

Electrophilic covalent warheads are valuable chemical probes in chemical biology for studying protein function and discovering new therapeutics. This poster describes the synthesis of sulfoximine-bicyclo[1.1.0]butanes (BCBs) as cysteine-selective chiral warheads…

Oxetanes are increasingly utilized motifs in drug discovery, however, remain to be validated. Their use as pendant motifs to attenuate amine basicity has led to increased interest in amino-oxetanes as design options…

Isocitrate dehydrogenase 1 (IDH1) overexpression occurs in a multitude of cancers and has been associated with decreased progression free survival in glioblastoma and high-grade serous ovarian cancer…