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The morpholine fragment is one of the most common amine moieties in drug design, valued for excellent solubility and permeability features. However, it also introduces metabolic liabilities, such as CYP-mediated oxidation, dealkylation, and ring opening. Its closest spirocyclic analogues, oxaazaspiro[3.3]heptanes (spiro morpholines), have recently shown strong potential in drug development, with several candidates currently in clinical trials. Enamine offers one of the most advanced and diverse collections of spiro morpholines, including isomeric structures and substitutions. The isomers enable variations in molecular dipole and pKa while retaining a molecular volume nearly identical to that of morpholine.

Spiro Morpholines

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Concept: Spiro Morpholines

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Over 25 oxaazaspiro[3.3]heptanes from stock on gram scale.

 

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