The spiropentyl substituent has gained traction in recent medicinal chemistry projects, not only for its elegant, bow-tie-like appearance but also for its highly desirable 3D structure. Recent studies from Merck demonstrate that this fragment enhances local hydrophobicity while resisting metabolic clearance—favorable traits for improving a drug’s pharmacokinetic profile. In July 2024, Vertex submitted a new drug application to the FDA for vanzacaftor, a molecule featuring the spiropentyl group, aimed at treating cystic fibrosis. Enamine offers an extensive selection of molecular building blocks with small spiro skeletons, spiropentane and dispiroheptane.
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Over 50 spiropentanes from stock on 5-10 gram scale.
