Process for preparing oxazolines from tetrahydrofurans

Details Process for preparing oxazolines from tetrahydrofurans Process for preparing oxazolines from tetrahydrofurans

C - Chemistry, Metallurgy

07

D

C07D 263/14 (2006.01) C07D 307/22 (2006.01) C07D 413/06 (2006.01)

Patent

CA 2387997

Methods for the preparation of chemical intermediates in the synthesis of HIV- protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrahydrofuran derivatives (II) into oxazolines (I) to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

L'invention concerne des procédés destinés à la préparation d'intermédiaires dans la synthèse d'inhibiteurs de la protéase du VIH concernant et comprenant du nelfinavir mesilate. Le procédé de cette invention consiste à transformer des dérivés de tetrahydrofuranne (II) en oxazolines (I) pour obtenir des intermédiaires réactionnels principaux destinés à la préparation de nelfinavir. L'invention concerne également un procédé destiné à la préparation d'un amino-alcool chiral à partir d'un époxy-tétrahydrofuranne.

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