Amr Technology, Inc.

Pfizer Corporation

Arthur E Harms

James Beck

Anthony D Pechulis

Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.

4-Phenyl substituted tetrahydroisoquinolines and therapeutic use thereof

4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof

4-phenyl substituted tetrahydroisoquinolines therapeutic use thereof

The invention provides a process for the optical resolution of a racemic mixture, or an optically enriched mixture, of trans-7-(hydroxymethyl)octa-hydro-2H-pyrido-1,2a)pyrazine, a key intermediate for preparing pharmacologically active 2,7-substituted octahydro-1H-pyrido&lsqb;1,2-a&rsqb;pyrazine derivatives useful in the treatment of disorders of the dopamine system. The process of the invention involves use of D-(&minus;) or L-(&plus;)naproxen as a resolving agent.

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Niskayuna, NY, United States of America

Arthur E Harms