Mallinckrodt, Inc.

Brian Orr

Keith G Tomazi

Gary Lee Cantrell

Tao Jiang

Christopher W Grote

Dennis J Kalota

Joseph P Haar, Jr

Esa T Jarvi

James R Meyer

Anthony Mannino

William E Dummitt

George H Klemm

Brenda E Allen

Miranda Steele

Jr Joseph Haar

The present disclosure generally related to an improved process for the preparation of various piperidine derivatives. More particularly, the present disclosure related to an improved process for preparing sufentanil base (1) and related compounds, which advantageously utilizes more cost effective and/or less hazardous reagents, including a dispersion comprising between about 50% and about 70% by weight (based on the total weight of the dispersion) of an alkali metal hydride, such as sodium hydride, as well as eliminates the need for expensive and/or time consuming purification techniques. 

Process for the preparation of sufentanil base and related compounds

The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.

Preparation of N-alkylated opiates by reductive amination

The present disclosure generally relates to methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydromorphone, hydrocodone, or a derivative thereof, by means of a non-catalytic hydrogenation reaction of thebaine, oripavine or a derivative thereof, respectively, using a hydrazide reagent, followed by hydrolysis of the hydrogenated intermediate at a low temperature and for a short period of time. Additionally, the present disclosure relates to a composition comprising the desired hydromorphone, hydrocodone, or a derivative thereof, in combination with a 6-beta compound that is structurally related thereto.

Methods for producing hydrocodone, hydromorphone or a derivative thereof

The present invention provides process for the production of opiate alkaloids. In particular, the present invention provides processes for the production of buprenorphine or a derivative of buprenorphine that minimizes the formation of impurities.

Processes for the production of buprenorphine with reduced impurity formation

The invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for the formation of opiate alkaloids that minimizes the formation of impurities.

Processes for the synthesis of opiates alkaloids with reduced impurity formation

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O'Fallon, MO, United States of America

Brian Orr