Process for preparing substituted 5-fluoro-1H-pyrazolopyridines
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 compound of formula (I) in crystalline form of polymorph I
wherein the x-ray diffractogram of the compound exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 22.7.
2. The compound of claim 1 , wherein the x-ray diffractogram of the compound exhibits peak maxima of the 2 theta angle at 5.9, 6.9, 16.2, 16.5, 24.1, 22.7, 24.7.
3. The compound of claim 1 , wherein the IR spectrum of the compound exhibits band maxima at 1707, 1633, 1475 cm −1 .
4. The compound of claim 3 , wherein the IR spectrum of the compound exhibits band maxima at 1707, 1633, 1566, 1475, 1255, 1223 cm −1 .
5. A process for preparing the compound of claim 1 , comprising:
stirring a solution of compounds of formula (I), wherein the compounds of formula (I) are present in one or more polymorphs or as a solvate in an inert solvent, at a temperature of 20° C.-120° C., and isolating the compound of formula (I) in the form of crystalline polymorph I from the solution.
6. A solid pharmaceutical composition comprising a compound of claim 1 and no greater proportion of any other form of the compound of the formula (I).
7. A solid pharmaceutical composition comprising a compound of claim 1 in more than 90 percent by weight based on the total amount any other form of the compound of the formula (I) present.
8. A method for treatment of cardiovascular disorders by administering an effective amount of the compound of claim 1 to a patient in need thereof.