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.
Taddei, M., Russo, A., Cini, E., Riva, R., Rasparini, M., Carcone, L., et al. (2011)Process for the production of aliskiren. . Brevetto No. WO 2011151442 A2.
Process for the production of aliskiren
TADDEI, MAURIZIO;RUSSO, ADELE;CINI, ELENA;
2011-01-01
Abstract
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.
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https://hdl.handle.net/11365/34218
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