Process for the preparation of enantiomerically enriched...

Details Process for the preparation of enantiomerically enriched... Process for the preparation of enantiomerically enriched...

C - Chemistry, Metallurgy

07

C

C07C 227/32 (2006.01) C07C 229/34 (2006.01) C07C 231/18 (2006.01) C07D 213/55 (2006.01) C07D 213/64 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2561973

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

La présente invention a trait à un procédé pour la préparation efficace de dérivés d'acides aminés bêta à enrichissement énantiomérique dans lequel le groupe aminé est non protégé. Les dérivés d'acides aminés bêta chiraux obtenus sont utiles dans la synthèse asymétrique de molécules biologiquement actives. Le procédé comprend une hydrogénation sélective d'un acide acrylique aminé bêta prochiral à amine non protégée ou un dérivé de celui-ci en présence d'un précurseur métallique à base de rhodium complexé avec un ligand monophosphine ou biphosphine chiral.

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