A spiro compound is a polycyclic compound in which two monocyclic rings share one carbon atom; the shared carbon atom is called a spiro atom. Spiro compounds have rigid structures, stable structures, and have special properties that general organic compounds do not possess, such as anomeric effect, spiro conjugation and spiro hyperconjugation. Compared with the monocyclic structure or the planar aromatic structure, the spiro structure has a larger three-dimensional structure; the heterocyclic spiro structure is also regarded as the biological isostere of some groups, which can change the drug to a certain extent. The water solubility, lipophilicity, dominant conformation and ADMET properties of the molecule make the optimized lead molecule easier to drug. Therefore, spiro compounds occupy a very important position in drug development.
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Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Tetrahydropyran is an organic compound consisting of a saturated six-membered ring containing five carbon atoms and one oxygen atom. Tetrahydropyrans are common structural motifs in natural products and synthetic therapeutic molecules. In nature, these six-membered oxygen heterocycles are usually assembled by intramolecular reactions, including oxygen Michael addition or ring opening of epoxy alcohols. In fact, polyether natural products have been particularly extensively studied for their fascinating structures and important biological properties; these are often formed through endoselective epoxy open cascades.
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