IP Library › Granted Patent US 10,633,357
Granted Patent B2
US 10,633,357 · App. 16/278,813 · Granted Apr 28, 2020

Intermediates and process for preparing intermediates in the production of substituted pyrazolopyridines

Inventor: Peter Fey (Wuppertal, DE)
Assignee: ADVERIO PHARMA GMBH
C07D295/104A61P9/00C07C303/28C07C309/04C07C317/04C07D265/30C07D295/067C07D471/04C07B2200/13
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Quick Facts
Patent No.
US 10,633,357
App. No.
16/278,813
Granted
Apr 28, 2020
Kind
B2
Abstract

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

Claims (13)

1. A process for preparing a compound of formula (IIIa)

comprising reacting the trifluoromethanesulphonic anhydride of the formula (X)

with 2,2,3,3-tetrafluoro-1-propanol of the formula XI,

without solvent, and

reacting the resulting 2,2,3,3-tetrafluoropropyl trifluoromethanesulphonate of the formula XII

with morpholine to give a compound of the formula (XIII)

and reacting the compound of formula (XIII) with methyl methane sulphonate to give a compound of the formula (XIV)

and with sodium hydroxide to give a compound of the formula (XV)

and finally adding morpholine to the compound of formula (XV) to give the compound of the formula (IIIa).

2. A compound of the formula (XIV)

and the salts, solvates and solvates of the salts thereof.

3. A compound of the formula (XV)

and the salts, solvates and solvates of the salts thereof.

Assignments (1)
CHANGE OF PATENTEE ADDRESS Recorded Feb 8, 2021
From: ADVERIO PHARMA GMBH
To: ADVERIO PHARMA GMBH
Reel/Frame 056907/0570 →
Priority Claims (2)
EP 11190789 · Nov 25, 2011 · regional
EP 11192301 · Dec 7, 2011 · regional
Continuity (6)
Division 15812524 · Nov 14, 2017
Division 15435964 · Feb 17, 2017
Division 14796703 · Jul 10, 2015
Division 14320875 · Jul 1, 2014
Division 13684670 · Nov 26, 2012
Related Publication 20190177288A1 · Jun 13, 2019