An approach for the diastereoselective synthesis of (R)‐(+)‐methyl pipecolate and (+)‐dextro‐erythrophacetoperane from (S)‐(−)‐methylbenzylamine

A diastereoselective synthesis for the preparation of ( R )‐methyl pipecolate and dextro‐erythrophacetoperane, analogs of methylphenidate, drugs used to treat attention deficit hyperactivity disorder, is reported. The key steps involve a high diastereoselective ring‐closing reaction via enolate formation and a diastereoselective ketone reduction reaction. The total synthesis of these valuable drugs could be obtained in only 5 and 8 steps, respectively, starting from ( S )‐(−)‐methyl benzylamine.