abstract |
The invention is concerned with a process for the manufacture of 3-amino-pyrrolidinenderivatives of the formulan n whereinn R 1 signifies hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an aminonprotecting group; and R 2 , R 3 each independently signify hydrogen, alkyl, cyclo-alkyl, alkenyl ornaryl; nby converting a compound of the formulan nwhereinn X signifies a protected hydroxy group; nin the presence of a primary amine of the formula R 1 NH 2 into the pyrrolidine derivative ofnthe formulan n wherein X and R 1 have the aforementioned significances; nwhich is subsequently reacted in the presence of R 2 R 3 NH under pressure. |