Carl Eugene Schaefer

US Patent:

8283472, Oct 9, 2012

Filed:

Jan 6, 2010

Appl. No.:

12/652894

Inventors:

Carl J. Schaefer - Crestwood MO, US
Charles S. Kuivila - St. Louis MO, US

Assignee:

Mallinckrodt LLC - Hazelwood MO

International Classification:

C07D 211/34

US Classification:

546238

Abstract:

A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as α-phenyl-α-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The α-phenyl-α-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.

US Patent:

20080319227, Dec 25, 2008

Filed:

Nov 27, 2006

Appl. No.:

12/096624

Inventors:

Sidney Liang - Olivette MO, US
John R. Duchek - St. Louis MO, US
Carl J. Schaefer - Crestwood MO, US

International Classification:

C07C 315/02

US Classification:

564162

Abstract:

The present invention generally relates to an improved process for preparing modafinil and analogs thereof. The process minimizes impurities and improves the overall yield by oxidizing a modafinil intermediate compound in a reaction mixture including an alcohol and an organic acid at a ratio of from about 1:1 to about 80:1 (by volume).

US Patent:

20110077222, Mar 31, 2011

Filed:

Sep 30, 2010

Appl. No.:

12/894203

Inventors:

Carl J. Schaefer - Crestwood MO, US
Gary L. Cantrell - Troy IL, US

Assignee:

Mallinckrodt Inc. - Hazelwood MO

International Classification:

A61K 31/485
C07F 9/09
A61P 25/04

US Classification:

514 81, 546 23

Abstract:

The present invention provides sustained-release opiate compositions. In particular, the present invention provides sustained-release opiate compositions that include an opiate attached to a blood albumin binder. The present invention also relates to methods of administering an opiate with a sustained release pharmacokinetic profile.