Method of preparing retroviral protease inhibitor intermediates

Details Method of preparing retroviral protease inhibitor intermediates Method of preparing retroviral protease inhibitor intermediates

C - Chemistry, Metallurgy

07

C

C07C 213/10 (2006.01) C07C 215/18 (2006.01) C07C 215/26 (2006.01) C07C 215/28 (2006.01) C07C 269/08 (2006.01) C07C 271/20 (2006.01) C07C 275/24 (2006.01) C07C 319/28 (2006.01) C07C 323/25 (2006.01) C07C 323/39 (2006.01) C07D 207/404 (2006.01) C07D 207/452 (2006.01) C07D 209/44 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2210973

Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

L'invention porte sur des isostères chiraux du type hydroxyéthylamine, hydroxyéthylurée ou hydroxyéthylsulfonamides contenant des protéases rétrovirales et des inhibiteurs de rénine pouvant se préparer par un procédé de synthèse multiétagée recourant à des intermédiaires clefs du type amines. Ladite invention est un moyen économique d'obtention desdites amines sous une forme chirale énantioméricalement, diastéréoméricalement et chimiquement pure. Le procédé est adapté à la production en masse (plusieurs kg). L'invention porte également sur les sels d'acides organiques et inorganiques des amines intermédiaires.

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