Process for the preparation of .alpha.-aminoketones

Details Process for the preparation of .alpha.-aminoketones Process for the preparation of .alpha.-aminoketones

C - Chemistry, Metallurgy

07

C

C07C 221/00 (2006.01) C07C 213/00 (2006.01) C07C 225/06 (2006.01) C07C 225/16 (2006.01) C07C 249/02 (2006.01) C07C 251/24 (2006.01) C07C 269/04 (2006.01) C07C 269/06 (2006.01) C07C 271/18 (2006.01) C07C 319/20 (2006.01) C07C 323/25 (2006.01) C07D 303/36 (2006.01) C07C 271/16 (2006.01)

Patent

CA 2361475

A process which comprises converting a .alpha.-amino acid ester into the corresponding imine to thereby protect the amino group of the ester, reacting the imine with a halomethyllithium to form an N-protected .alpha.-amino halomethyl ketone, and treating this N-protected .alpha.-amino halomethyl ketone with an acid to obtain a .alpha.-amino halomethyl ketone. This process is suitable for industrial production and permits economical and efficient production of .alpha.-amino halomethyl ketones and compounds related thereto.

L'invention concerne un procédé qui consiste à convertir un ester d'alpha-aminoacide en imine correspondante, de manière à protéger le groupe amino de l'ester. On fait réagir l'imine avec un halométhyllithium pour former une alpha-amino halométhyl-cétone à protection N, qui est ensuite traitée avec un acide de manière à donner une alpha-amino halométhyl-cétone. Ce procédé est approprié à la fabrication industrielle et permet d'assurer une production économique et efficace d'alpha-amino halométhyl-cétones et de composés connexes.

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