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The stereoselective synthesis of the non‐lactonic part of the natural G2 checkpoint inhibitor, (Z)‐cryptofolione, has been accomplished. Butane‐1,4‐diol was used as the starting material, and the stereogenic centers were generated through L‐proline‐catalyzed α‐aminoxylation and Maruoka asymmetric allylation. We attempted to convert this non‐lactonic moiety to (Z)‐cryptofolione via olefin cross‐metathesis reaction, but by this approach another naturally occurring lactonic compound, goniothalamin, was obtained.

2-Naphthol underwent Friedel-Crafts reaction with Nbenzyloxycarbonylamino sulfones in the presence of InCl 3 at room temperature to form the corresponding sulfonyl derivatives in high yields. The products were subsequently reacted with nucleophiles such as allyltributyltin and anisole to replace the sulfonyl group.