Intermediates and process for preparing intermediates in the production of substituted pyrazolopyridines
View Patent ↗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.
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.