PROCESS FOR PREPARING SUBSTITUTED 5-FLUORO-1H-PYRAZOLOPYRIDINES

Abstract

The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI)

##STR00001##

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)

##STR00002##

which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.

Claims

1.-3. (canceled)

4. A process for preparing an aldehyde of formula (III) ##STR00085## in which R.sup.1 and R.sup.2 are each independently methyl, ethyl, isopropyl, phenyl or, together with the nitrogen atom to which they are bonded, are ##STR00086## comprising reacting trifluoromethanesulphonic anhydride with 2,2,3,3-tetrafluoro-1-propanol, without solvent, and reacting the resulting 2,2,3,3-tetrafluoropropyl trifluoromethanesulphonate with a compound of formula (XIIa) ##STR00087## in which R.sup.1 and R.sup.2 are each as defined above to give a compound of formula (XIIIa) ##STR00088## in which R.sup.1 and R.sup.2 are each as defined above and reacting the compound of formula (XIIIa) with methyl methanesulphonate to give a compound of the formula (XIVa) ##STR00089## in which R.sup.1 and R.sup.2 are each as defined above and reacting the compound of (XIVa) with sodium hydroxide to give a compound of formula (XVa) ##STR00090## in which R.sup.1 and R.sup.2 are each as defined above and reacting the compound of formula (XVa) with a compound of the formula (XIIa) to give the compound of formula (III).

5.-26. (canceled)

Description

FIGURES

[0331] FIG. 1: IR spectrum of the compound of the formula (I) in polymorphs I, II and III

[0332] FIG. 2: IR spectrum of the compound of the formula (I) in polymorphs IV, V and as the triacetic acid solvate

[0333] FIG. 3: IR spectrum of the compound of the formula (I) as the di-DMSO solvate, DMF/water solvate and monohydrate

[0334] FIG. 4: IR spectrum of the compound of the formula (I) as the dihydrate

[0335] FIG. 5: X-ray diffractogram of the compound of the formula (I) in polymorph I

[0336] FIG. 6: X-ray diffractogram of the compound of the formula (I) in polymorph II

[0337] FIG. 7: X-ray diffractogram of the compound of the formula (I) in polymorph III

[0338] FIG. 8: X-ray diffractogram of the compound of the formula (I) in polymorph IV

[0339] FIG. 9: X-ray diffractogram of the compound of the formula (I) in polymorph V

[0340] FIG. 10: X-ray diffractogram of the compound of the formula (I) as the triacetic acid solvate

[0341] FIG. 11: X-ray diffractogram of the compound of the formula (I) as the di-DMSO solvate

[0342] FIG. 12: X-ray diffractogram of the compound of the formula (I) as the DMF-water solvate

[0343] FIG. 13: X-ray diffractogram of the compound of the formula (I) as the monohydrate

[0344] FIG. 14: X-ray diffractogram of the compound of the formula (I) as the dihydrate