| 摘要 |
<p>The present invention relates to a process for the preparation of a N-(N'-substituted glycyl)- 2 -cyanopyrrolidine comprising at least (a) reacting, in the presence of dimethylformamide, a compound of formula (V) wherein, independently of each other, X<SUB>1 </SUB>and X<SUB>3 </SUB>are halogen; X<SUB>2 </SUB>is halogen, OH, O-C(-O)-CH<SUB>2</SUB>X<SUB>3</SUB>, -O-SO<SUB>2</SUB>-(C<SUB>1-8</SUB>)alkyl or 13 O-SO<SUB>2</SUB>-(aryl), with L-prolinamide, followed by (b) reacting the resultant compound without isolation with a dehydration agent, optionally followed by (c) reacting, in the presence of a base, the resultant compound without isolation with an appropriate amine and (d) recovering the resultant compound in free form or in acid addition salt form.</p> |
