Warner-lambert Company

Marvin Simon Hoekstra

Om Prakash Goel

Thomas F Mich

James Andrew Ramsden

Thomas Mulhern

Mark Joseph Burk

This invention provides a method of making (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid (pregabalin) or a salt thereof via an asymmetric hydrogenation synthesis. Pregabalin is useful for the treatment and prevention of seizure disorders, pain, and psychotic disorders. The invention also provides intermediates useful in the production of pregabalin.

Asymmetric synthesis of pregabalin

The preparation of Bevantolol--i.e., 1-[ 3,4-dimethoxyphenethylamine] -3-(m-tolyloxy)-2-propanol--is facilitated by contacting the reactants at relatively low temperatures.

Bevantolol preparation

Dihydro-1H-pyrrolizine-3,5-(2H,6H)-dione is produced in higher overall yield in a process which comprises catalytically hydrogenating a lower alkyl ester of 4-(hydroxyimino)heptanedioic acid in the presence of a tri-(lower alkyl)amine, followed by cyclization of the product thus produced in the presence of a cyclizing agent such as acetic anhydride.

Growing community of inventors

Holland, MI, United States of America

Marvin Simon Hoekstra