The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Dec. 21, 1999
Filed:
Sep. 02, 1997
Richard J Martin, San Jose, CA (US);
John D Stilger, San Jose, CA (US);
Mark R Holst, Concord, CA (US);
John D Young, Falkirk, GB;
Michael P Barkdoll, Knoxville, TN (US);
Bradley L Edgar, Berkeley, CA (US);
Thermatrix, Inc., San Jose, CA (US);
Abstract
A process is provided for preparing oxymorphone from morphine by: (1) reacting morphine with (1a) an acyl halide or anhydride to form 3-acylmorphine, or (1b) reacting morphine with benzyl-halide to form 3-benzylmorphine; (2) Oxidizing the 6-hydroxy group of the 3-acyl or 3-benzylmorphine so as to form the corresponding 3-acyl or 3-benzylmorphinone; and thereafter either by (3a) or (3b): (3a) introducing a .beta.-oriented hydroxy group at the 14-position of the 3-acyl- or 3-benzyl-morphinone with aqueous hydrogen peroxide and an acid at a temperature of about 15.degree. to about 70.degree. C. to form the 3-acyl or 3-benzyl-14-hydroxymorphinone; (3b) acylating the 3-acyl or 3-benzyl-morphinone with an acylating agent so as to form the dienol acylate followed by oxidizing the dienol acetate to the corresponding 3-acyl or 3-benzyl-14 -hydroxymorphinone; (4) hydrogenating the 3-acyl-14-hydroxymorphinone with a catalyst so as to form the 3-acyloxymorphone; (5) hydrolyzing the 3-acyl-oxymorphone with aqueous acidic or basic solution to form oxymorphone; (6) hydrogenating the 3-benzyl-14-hydroxymorphinone with a catalyst so as to form oxymorphone.