IP Library › Granted Patent US 11,040,953
Granted Patent B2
US 11,040,953 · App. 16/939,976 · Granted Jun 22, 2021

Process for the preparation of a diarylthiohydantoin compound

Inventors: Cyril Ben Haim (Beerse, BE); Andras Horvath (Turnhout, BE); Johan Erwin Edmond Weerts (Beerse, BE); Jennifer Albaneze-Walker (Mol, BE)
Assignee: Aragon Pharmaceuticals, Inc.
C07D401/04B01J31/24B01J31/26C07B43/06C07D213/61C07D213/84C07D233/86C07D235/02
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Quick Facts
Patent No.
US 11,040,953
App. No.
16/939,976
Granted
Jun 22, 2021
Kind
B2
Abstract

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

Claims (6)

1. A process for preparing compound 1c:

the method comprising converting compound VII to compound 1c:

2. The process of claim 1 comprising:

reacting compound VII with an organomagnesium halide; in the presence or absence of a lithium halide; and

adding carbon dioxide gas; in an aprotic organic solvent; at a temperature of about 0° C. to yield compound 1c.

3. The process of claim 1 , comprising reacting compound VII under a carbon monoxide atmosphere; in the presence of a palladium catalyst; in the presence of one or more phosphorus ligands; in the presence of water; in a solvent; at a temperature of about 0° C. to about 100° C. to yield the compound 1c.

Continuity (4)
Continuation 16427637 · May 31, 2019
Continuation 15537859
Provisional Application 62094425 · Dec 19, 2014
Related Publication 20200354334A1 · Nov 12, 2020