The stereocontrolled synthesis of atorvastatin calcium starting from commercially available d‐aspartic acid using an intramolecular oxidative oxygen‐nucleophilic bromocyclization of a homoallylic tert‐butyl carbonate is described. This strategy allows the formation of the chiral syn‐1,3‐diol moiety with the desired stereochemistry, and provides a functionalized bromomethyl group for the construction of the atorvastatin side‐chain with high regio‐ and diastereoselectivity. This route is attractive as it represents an efficient and environmentally sensitive approach to the large‐scale synthesis of statins and their analogues.

No abstract

No abstract