New scaffolds for drug discovery, 6‐azaspiro[4.3]alkanes, have been synthesized in two steps from four‐membered‐ring ketones: cyclobutanone, thienone, N‐Boc‐azetidinone (Boc = tert‐butoxycarbonyl), etc. The key transformation was the reaction between electron‐deficient exocyclic alkenes and an in‐situ generated N‐benzylazomethine ylide.

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A convenient approach towards enantiopure (R) and (S) isomers of 2,2,2‐trifluoro‐1‐(heteroaryl)ethanols was developed. The enzyme‐catalyzed kinetic resolution of the corresponding racemic mixtures was achieved by using a two‐step protocol that involved an acylation and a hydrolysis step in the presence of Burkholderia cepacia and CAL‐B lipase (Candida antarctica lipase B), respectively. Fourteen compounds were resolved on a multigram scale by using this approach. The observed enantioselectivities correlated well with the results of molecular docking experiments.