Process for the preparation of 3-amino-pyrrolidine derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 207/14 (2006.01) C07D 401/00 (2006.01) C07D 403/00 (2006.01) C07D 501/00 (2006.01) C07D 501/04 (2006.01) C07D 501/24 (2006.01)

Patent

CA 2258166

The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula Image wherein R1 signifies hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and R2, R3 each independently signify hydrogen, alkyl, cyclo-alkyl, alkenyl or aryl; by converting a compound of the formula Image wherein X signifies a protected hydroxy group; in the presence of a primary amine of the formula R1NH2 into the pyrrolidine derivative of the formula Image wherein X and R1 have the aforementioned significances; which is subsequently reacted in the presence of R2R3NH under pressure; and with the use of this process for the production of vinylpyrrolidinone-cephalosporin derivatives.

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