Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory drugs.
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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