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US 7,741,490 B2Granted
Intermediates for the preparation of pramipexole
AssigneeDipharma S.p.A.
InventorsGraziano Castaldi, Alberto Bologna, Pietro Allegrini, Gabriele Razzetti, Vittorio Lucchini
Life of this patent
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Abstract
Intermediates useful for the preparation of pramipexole and the use thereof in such synthesis.
Claims2
A process for the preparation of pramipexole, or a pharmaceutically acceptable salt thereof, comprising the acylation of a compound of formula (VII), either as the single (S) enantiomer or as mixture of (R,S) enantiomers
- wherein R3 is hydrogen and Ra is a free or protected amino group, by reaction with propionic anhydride, and subsequent reduction of the resulting compound of formula (IX)
- wherein Ra is as defined above, by treatment with an alkali metal borohydride and molecular iodine, to obtain a compound of formula (VIII)
- wherein R3 is hydrogen and Ra is as defined above;
- followed, if necessary, by deprotection of the primary amino group and/or by resolution of the mixture of (R,S) enantiomers into the single (S) enantiomer and, if desired, by conversion of pramipexole to a pharmaceutically acceptable salt thereof.
1 more element
Dependencies are inferred from the claim text.