Mallinckrodt, Inc.

Edmund C Hudson

Gary Lee Cantrell

Peter Xianqi Wang

Christopher W Grote

Subo Liao

Esa T Jarvi

Catherine E Thomasson

John Brandt

Michael Schaefer

Sharon Woods

Douglas Teramura

The invention generally provides processes for the preparation of radioiodinated 3-fluoropropyl-nor-&#x3b2;-CIT. In particular, the process uses an arylsilane intermediate, thus avoiding the use of hexamethylditin, and reducing the number of steps previously required for the preparation of radioiodinated 3-fluoropropyl-nor-&#x3b2;-CIT from anhydroecgonine methyl ester. The invention also relates to the alkylation of a nortropane to the corresponding N-(3-fluoropropyl) analog using 3-fluoropropanal.

Process for the preparation of radioiodinated 3-fluoropropyl-nor-&#x3b2;-CIT

The present invention provides processes for preparing normorphinans from N-substituted morphinans. In particular, the invention provides methods for removing the N-substituent from the N-substituted morphinan to from a normorphinan carbamate, and then removing the carbamate functionality from the normorphinan carbamate to form the normorphinan.

Preparation of normorphinans

The invention provides a process for the N-alkylation of normorphinan compounds to produce N-alkylated morphinan compounds. In particular, the process relates to the alkylation of a normorphinan compound by a carboxaldehyde in the presence of a reducing agent to form an N-alkylated morphinan.

Process for the reductive alkylation of normorphinans

The present invention is generally directed to a process for the preparation of a ketomorphinan comprising maintaining a ketone group as unprotected and performing reductive amination using a hydrogen source and a catalyst.

Processes for the selective amination of ketomorphinans

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Clayton, MO, United States of America

Edmund C Hudson