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A NEW, EFFICIENT AND ECONOMIC METHOD FOR PREPARATION OF PRAMIPEXOLE.
|Roman Balicki , Agnieszka Ciesielska , Michał Odrowąż-Sypniewski
Pharmaceutical Research Institute (IF), Rydygiera 8, Warszawa 01-793, Poland
Pramipexole is a novel nonergot dopamine agonist which has high selectivity for interacting with dopamine D2 receptors. It is effective in early Parkinson,s disease as monotherapy and as adjunctive therapy with L-dopa in advanced stages of the disease.
Known, two-steps method for preparation of pramipexole (3) is based on acylation reaction of diamine 1 with propionic anhydride. The obtained amide 2 is subsequently reduced using borane to give final product 3 with 65% yield.
Now, we present novel, more economic and safe procedure for obtaining pramipexole. Our one-step method requires only alkylation of 1 using n-propyl tosylate. Dangerous reduction with borane is eliminated and the final compound is obtained with similar yield as in a previous method.
Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Agnieszka Ciesielska
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku
Submitted: 2006-01-26 16:30 Revised: 2009-06-07 00:44