Synthesis of Chiral Amphetamine Derivatives by Stereospecific, Regioselective Cuprate Addition Reaction with Aziridine Phosphoramidate Compounds

摘要

The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions,

主权项

1. A process of making the dexamphetamine, said process comprising:
providing a compound of Formula 5 having a regioisomeric purity >99%:wherein R is alkyl or aryl; and
deprotecting the compound of Formula 5 under acidic conditions effective to produce dexamphetamine of Formula I: