NOVEL PREGABALIN INTERMEDIATES AND PROCESS FOR PREPARING THEM AND PREGABALIN

The present invention provides novel compounds, which are especially useful as intermediates for the preparation of Pregabalin. The invention also relates to process for preparing these intermediates and Pregabalin

Sviluppo di un nuovo processo per la sintesi di Aliskiren [Process development of generic Aliskiren]

A synthesis of the new-generation antihypertensive Aliskiren is described. This innovative process features an asymmetric hydrogenation to simultaneously control two of the four chiral centers and a strategic use of the Curtius rearrangement

Process for the production of aliskiren

The invention relates to a process for the prepn. of aliskiren (I), using enzymic hydrolysis and catalyzed hydrogenation as key steps. The process for prepg. aliskiren comprising enzymic hydrolysis of II in the presence of pig liver esterase or liver acetone powder obtained from ovis, bovine and equine, is claimed. Compd. I was prepd. by enantioselective enzymic hydrolysis of II, followed by redn. to alc., iodination and alkylation with III; the resulting β-dicarbonyl compd. underwent acylation/dehydration followed by rhodium-catalyzed hydrogenation, hydrolysis, rearrangement to amine and intramol. condensation to give IV, which underwent ring opening/amidation with 3-amino-2,2-dimethylpropanamide and hydrolysis to give I