Amine salts of pitavastatin and rosuvastatin
View Patent ↗The present invention relates to oxygen-comprising amine salts of HMG-CoA reductase inhibitors, to a method of producing said amine salts and to the use of said amine salts in the production of pharmaceutically acceptable salts of HMG-CoA reductase inhibitors.
1. An amine salt of pitavastatin or rosuvastatin, wherein the amine comprises an ethyldiethanol amine.
2. The amine salt of claim 1 , wherein the ethyldiethanol amine is 2,2′-(ethylenedioxy)diethyl amine.
3. The amine salt of claim 2 which is the 2,2′-(ethylenedioxy)diethyl amine di-salt of rosuvastatin.
4. A method for the preparation of the amine salt of claim 1 comprising the steps of:
a) contacting a protected derivative of pitavastatin or rosuvastatin with acid followed by base or with base followed by acid;
b) treating the mixture obtained in step a) with an ethyldiethanol amine; and
c) isolating the amine salt obtained in step b).
5. The method of claim 4 , wherein step a) is practiced with the protected derivative of rosuvastatin and step b) is practiced with 2,2′-(ethylenedioxy)diethyl amine to thereby form the 2,2′-(ethylenedioxy)diethyl amine di-salt of rosuvastatin which is isolated according to step c).