Processes and intermediates for the preparation of Pimavanserin

• US 10,343,993 B2
• Filed: 03/02/2016
• Issued: 07/09/2019
• Est. Priority Date: 03/02/2015
• Status: Active Grant

• Current Assignee: Pliva Hrvatska doo (Teva Pharmaceutical Industries Limited)
• Original Assignee: Pliva Hrvatska doo (Teva Pharmaceutical Industries Limited)
• Inventors: Biljan, Tomislav, Dogan, Jasna, Metsger, Leonid, Pipercic, Sara Morasi, Ratkaj, Marina, Skugor, Maja Matanovic, Wang, Yi
• Primary Examiner(s): Reese, Heidi
• Application Number:
  US15/555,092
• Publication Number:
  US 20180037549A1
• Time in Patent Office: 1,224 Days
• Field of Search: None
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: C07B 2200/13 Crystalline forms, e.g. polymorphs
• CPC Class Codes: C07C 259/06 having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
• CPC Class Codes: C07C 269/04 from amines with formation of carbamate groups
• CPC Class Codes: C07C 271/48 to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• CPC Class Codes: C07D 211/58 attached in position 4
• CPC Class Codes: C07D 233/60 with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
• CPC Class Codes: C07D 233/61 with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
• CPC Class Codes: C07D 273/01 having one nitrogen atom

Abstract

The present disclosure relates to novel, safe and efficient processes for the synthesis of Pimavanserin and salts thereof, as well as novel intermediates that can be used in these processes.

Claims

1. A compound of formula (XVII), (Z), or (XIX):

2. The compound of formula (XVII) of claim 1, that is:

3. The compound of formula (Z) of claim 1, that is:

4. The compound of formula (XIX) of claim 1, wherein R¹ is 2-methylpropan-oxy.