Recent medicinal chemistry projects frequently use spirocyclic linkers to enhance molecular three-dimensionality and reduce metabolic susceptibility. A notable example is the family of spirocyclic azetidines, found in 5 approved drugs and 19 clinical trial candidates. However, crystal structure analyses often reveal crystallographic water in binding sites, suggesting a room for small substituents like methyl groups. To date, Deglocitinib, a Janus kinase inhibitor FDA-approved in 2025 for chronic hand eczema, is the only drug exemplifying the "magic methyl" concept in spiroazetidines. With Enamine now supplying a battery of methylated and other substituted derivatives, we anticipate more structures adopting this design.
Crystal Structures
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Over 50 methyl spiroazetidines from stock on 5-10 gram scale.
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