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.
Dioxolane is a heterocyclic acetal with the formula (CH2)2O2CH2. It is related to tetrahydrofuran by exchanging an oxygen for the CH2 group. The isomer 1,2-dioxolane (in which the two oxygen centers are adjacent) is a peroxide. 1,3-Dioxolane is used as solvent and comonomer in polyacetal. The dioxolane-type and their hydrogenolysis can provide very valuable partially protected building blocks either for oligosaccharide syntheses or sugar transformations.
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