A preparatively accessible route to a series of conformationally-locked bicyclic morpholines has been developed. This flexible approach allows for diversification in order for a small array of lead-like scaffolds to be synthesised from readily available key building blocks.

A diastereoselective Strecker reaction using (R)-(−)-phenylglycinol forms the basis of a concise scalemic route to dialkylhydantoin 1. The phenylglycinol functionality was exploited in the manipulation of the aminonitrile Strecker product through to the dialkylhydantoin via a short, efficient sequence involving crystalline intermediates.

A preparatively accessible route to a series of conformationally-locked bicyclic morpholines has been developed. This flexible approach allows for diversification in order for a small array of lead-like scaffolds to be synthesised from readily available key building blocks.