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.
Benzene is an important organic compound with the chemical formula C6H6, and its molecule consists of a ring of 6 carbon atoms, each with 1 hydrogen atom. Benzene is a sweet, flammable, colorless and transparent liquid with carcinogenic toxicity at room temperature, and has a strong aromatic odor. It is insoluble in water, easily soluble in organic solvents, and can also be used as an organic solvent itself. The ring system of benzene is called benzene ring, and the structure after removing one hydrogen atom from the benzene ring is called phenyl. Benzene is one of the most important basic organic chemical raw materials. Many important chemical intermediates can be derived from benzene through substitution reaction, addition reaction and benzene ring cleavage reaction.
Azetidines are an important class of saturated four-membered nitrogen-containing heterocyclic compounds. The research hotspots related to this structure mainly focus on two aspects: one is the research of pharmaceutical chemistry; the other is related to chiral azetidines, using rigid azetidine compounds as chiral ligands for asymmetric catalytic reactions. Many nitrogen-containing heterocycles play important roles in drug structures, and in many cases small structural changes can improve ligand selectivity and pharmacokinetic properties.
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