Meet a new weekend article - ‘Which boronic acids are used most frequently for the synthesis of bioactive molecules?’.   

In addition, we have created a nice selection of Heteroaromatic Boronic Acids Set.

Boronic acids (BAs) are very common building blocks used for the synthesis of bioactive molecules in medicinal chemistry. They are mainly used as reagents in coupling reactions like Suzuki-Miyaura, Chan-Lam, etc. It should be noticed that Suzuki reaction was the 2nd most used reaction to create libraries (after amide couplings) and BAs were used as the most frequent building block after carboxylic acids and amines. Another importance of BAs is caused also by application as active agents themselves. Thanks to the possibility of forming diols, BAs can be used as saccharide sensors, for example in the detection of glucose in diabetes patients.    

BAs from 3 large data sources were extracted. As a result - 11,245 unique boronic acids. They are suggested as a basis for library design for the efficient exploration of structure–activity relationships. A Boronic Acid Navigator was created by @Peter Ertl and is available at this link.   

The full article you can find here.

Great article! Many thanks to the authors - Peter Ertl, Eva Altmann, Sophie Racine, and Odile Decoret.