Piperidine is an azacycloalkane that is cyclohexane in which one of the carbons is replaced by a nitrogen. Although piperidine is a common organic compound, it is an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.
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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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The molecular structure of cyclobutane has four carbon atoms, and its four carbon atoms are not in the same plane, which is the folded conformation of cyclobutane. Cyclobutane itself is not of commercial or biological interest, but more complex derivatives are important in biology and biotechnology. Currently, nine FDA-approved drugs contain the cyclobutane structure. From the perspective of therapeutic areas, cyclobutyl drugs are mainly distributed in popular areas such as tumors, neurological diseases, infectious diseases, endocrine and metabolic diseases.
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