Making square drug fragments under pressure

cyclobutanen

Beeld: Daniël Linzel, Canva.com

1,2-substituted cyclobutanes can be easily prepared under high pressure and are interesting building blocks for drug development, a team from Nijmegen shows in the European Journal of Organic Chemistry.

In addition to the synthesis of complete drugs, chemists are also involved in so-called fragment-based drug discovery. This involves the production of small (reactive) fragments that can be used as ‘building blocks’ in the molecular design of drugs, allowing the rapid testing of specific structures. The group of Floris Rutjes (Radboud University), together with colleagues from Symeres and VU Amsterdam, synthesised a small library of what they considered to be an underrepresented structure: 1,2-disubstituted cyclobutanes.

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