Methods of producing molindone and its salts

Patent metadata

Field	Value
Publication number	US-11117862-B2
Application number	US-202016863020-A
Country	US
Kind code	B2
Filing date	Apr 30, 2020
Priority date	Sep 14, 2012
Publication date	Sep 14, 2021
Grant date	Sep 14, 2021

Abstract

The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

First claim

The invention claimed is:

1. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient, formaldehyde, and 2,3-pentanedione-2,3-dioxime.

2. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient, formaldehyde, 2,3-pentanedione-2,3-dioxime, and acetaldehyde oxime.

3. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient and 2,3-pentanedione-2,3-dioxime.

4. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient, 2,3-pentanedione-2,3-dioxime, and acetaldehyde oxime.

5. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient, 2,3-pentanedione-2,3-dioxime, acetaldehyde oxime, and 1-hydroxy-propan-2-one oxime.

6. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient and acetaldehyde oxime.

7. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient, acetaldehyde oxime, and 1-hydroxy-propan-2-one oxime.

8. A composition comprising molindone or its pharmaceutically acceptable salt as the sole active ingredient and 1-hydroxy-propan-2-one oxime.

Assignees

• Supernus Pharmaceuticals Inc

Inventors

• Hanbauer Martin
• Nazir Zarghun
• Hildebrand Peter
• Figini Attilia
• Liang Likan
• Fumagalli Tiziano

Classifications

• C07C249/08 Primary

  by reaction of hydroxylamines with carbonyl compounds · CPC title

• C07D209/08 Primary

  with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring · CPC title

• C07D295/13

  to an acyclic saturated chain · CPC title