Process for the preparation of...

C - Chemistry – Metallurgy – 07 – D

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C07D 209/54 (2006.01)

Patent

CA 2634397

The present invention provides for a process for preparing racemic methyl 6,6- dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3- azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid ("D-DTTA") salt or a (2R, 3S, 4R)-methyl 6,6- dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt ("L-DTTA") in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid ("D-DBTA") salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid ("L-DBTA") salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

La présente invention concerne un procédé pour la préparation de 6,6-diméthyl-3-azabicyclo[3,1,0]hexane-2-carboxylate de méthyle racémique, son sel correspondant : sel (2S, 3R, 4S)-méthyl 6,6-diméthyl-3-azabicyclo[3,1,0]hexane-2-carboxylate de l'acide di-p-toluoyl-D-tartarique ('D-DTTA') ou sel (2R, 3S, 4R)-méthyl 6,6-diméthyl-3-azabicyclo[3,1,0]hexane-2-carboxylate de l'acide di-p-toluoyl-L-tartarique ('L-DTTA') en excès énantiomérique élevé. La présente invention concerne également un procédé pour la préparation d'un sel (2S, 3R, 4S)-méthyl 6,6-diméthyl-3-azabicyclo[3,1,0]hexane-2-carboxylate de l'acide dibenzoyl-D-tartarique ('D-DBTA') ou sel (2R, 3S, 4R)-méthyl 6,6-diméthyl-3-azabicyclo[3,1,0]hexane-2-carboxylate de l'acide L-tartarique ('L-DBTA') en excès énantiomérique élevé. De plus, la présente invention concerne un procédé pour la préparation d'intermédiaires II, IIB, III, IV, sel IV, V, VI et VII.

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