Mallinckrodt, Inc.

Specgx LLC

Joseph P McClurg

Gary Lee Cantrell

Christopher W Grote

Frank William Moser

Bobby N Trawick

Subo Liao

Catherine E Thomasson

Tao Jiang

Peter Xianqi Wang

David W Berberich

John E Johnson, Jr

Sarah M Farris

Todd Osiek

Jr John E Johnson

The invention provides methods for preparing substituted phenylalkanes. In particular, the processes comprise reacting a phenyl boronic compound with an &#x3b1;-&#x3b2; unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction. The processes may be useful in the synthesis of tapentadol.

Process for preparing substituted phenylalkanes

The present invention provides compositions of 6-amino morphinan compounds and process for their synthesis. In particular, the processes provide for the reductive amination of 6-keto morphinans by catalytic transfer hydrogenation, to produce 6-amino morphinan compounds, which are epimerically and/or diastereomerically enriched.

Reductive amination of 6-keto morphinans by catalytic hydrogen transfer

The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catalytic hydrogen transfer.

Preparation of 6-alpha-amino N-substituted morphinans by catalytic hydrogen transfer

The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation.

Reductive amination of 6-keto normorphinans by catalytic hydrogen transfer

The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone.

Process and compounds for the production of (+)opiates

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Manchester, MO, United States of America

Joseph P McClurg