The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formula
wherein
R1signifies hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and
R2, R3each independently signify hydrogen, alkyl, cyclo-alkyl, alkenyl or aryl;
by converting a compound of the formula
wherein
Xsignifies a protected hydroxy group;
in the presence of a primary amine of the formula R1NH2 into the pyrrolidine derivative of the formula
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.
本发明涉及一种制造
3-氨基吡咯烷衍
生物的工艺,其式为
式中
R1 表示氢、烷基、环烷基、烯基、芳基或
氨基保护基团;和
R2、R3 各自独立地表示氢、烷基、环烷基、烯基或芳基;
将以下式子的化合物转化为
其中
X 表示受保护的羟基;
在式 R1NH2 的
伯胺存在下转化成式中的
吡咯烷衍
生物
其中 X 和 R1 具有上述意义;
然后在 R2R3NH 的存在下加压反应;以及使用该工艺生产
乙烯基吡咯烷酮-
头孢菌素衍
生物。