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Rozzano, Italy

Ferraboschi P.,University of Milan | Ciceri S.,University of Milan | Grisenti P.,EUTICALS SpA
Tetrahedron Asymmetry | Year: 2013

The synthetic antithrombotic argatroban is a dipeptide between the nonproteogenic (2R,4R)-4-methyl-2-piperidine carboxylic acid and l-arginine, in turn bonded to a 3-methyltetrahydroquinoline sulfonyl group; the drug is usually prepared and administered as a mixture of C-21-diastereoisomers. By means of a biocatalytic transformation enantiomerically pure (R)- and (S)-synthons, suitable for the synthesis of separate (21R)- and (21S)- argatroban, were obtained. © 2013 Elsevier Ltd. All rights reserved. Source


Ferraboschi P.,University of Milan | Ciceri S.,University of Milan | Ciuffreda P.,University of Milan | De Mieri M.,University of Milan | And 2 more authors.
Tetrahedron Asymmetry | Year: 2014

A biocatalyzed reduction of a prochiral bicyclic ketone afforded enantiomerically pure (R)-2-acetylamino-6-hydroxy-4,5,6,7-tetrahydrobenzothiazole, a synthon of the anti-Parkinson (S)-pramipexole and its (R)-isomer, which is currently under investigation for the treatment of amyotrophic lateral sclerosis (ALS). © 2014 Elsevier Ltd. All rights reserved. Source


Ferraboschi P.,University of Milan | Mieri M.D.,University of Milan | Grisenti P.,EUTICALS SpA | Lotz M.,Solvias AG | Nettekoven U.,Solvias AG
Tetrahedron Asymmetry | Year: 2011

The synthetic antithrombotic argatroban is a dipeptide between the nonproteogenic (2R,4R)-4-methyl-2-piperidine carboxylic acid and l-arginine, in turn bonded to a methyltetrahydroquinoline sulfonyl group. An extensive screening of transition metal-based complexes with different ligands was performed in order to identify the best catalyst for the diastereoselective hydrogenation of a suitable 4,5-dehydropiperidine precursor aimed toward a synthesis of the (2R,4R)-4-methyl piperidine moiety. Copyright © 2011 Published by Elsevier Ltd. All rights reserved. Source


Patent
Euticals S.p.A. | Date: 2015-10-07

A process for the preparation of the amorphous form of Regadenoson of formula is disclosed together with new crystalline polymorphic forms E, F and G and methods for their preparation. Regadenoson amorphous form can be prepared in mild reaction conditions with high chemical purity (>99.6%) and high stability to the heating. A particularly thermodynamically stable anhydrous crystalline form of Regadenoson (form G) is also disclosed, provided with high stability not when exposed to 90% RH at 25 C. for 96 hour, but also to the heating up to 200 C.


This invention relates to new water-soluble solid pharmaceutical inclusion complexes and their aqueous solutions for oral, ophthalmic, topical or parenteral use containing a macrolide and certain cyclodextrins. More particularly the invention relates to new water-soluble solid pharmaceutical inclusion complexes and their solutions in aqueous solvents, said compositions containing

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