What is it about?

We developed a chemical strategy (a sequence of reactions) to introduce on a steroid (pregnane) backbone different chemical groups (molecular diversity). The new steroid derivatives possess an additional ring with key substituents having different orientations. All new steroid derivatives were fully characterized to confirm the right structure.

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Why is it important?

To develop new drugs, the medicinal chemists must modify (diversify) small molecules with different scaffolds in order to introduce key substituents (chemical groups), which will be able to generate interactions with a therapeutic target (enzyme, receptor or protein). The strategy we developed will be useful to introduce a molecular diversity (small chemical groups) on different scaffolds having a ketone.

Perspectives

This strategy of diversification could be extended to different kinds of ketones, not just steroid ketones as illustrated with pregnenolone.

Dr Donald Poirier
Universite Laval

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This page is a summary of: Introducing Molecular Diversity at the C20-position of Pregnenolone by the Formation of Spiro-2-morpholinones, Current Organic Synthesis, June 2018, Bentham Science Publishers,
DOI: 10.2174/1570179414666171107161304.
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