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Aðferð til að framleiða N-útskipt 2-sýanópýrrólídín
专利权人:
Novartis AG
发明人:
Frank Schäfer,Gottfried Sedelmeier
申请号:
IS8122
公开号:
IS2979B
申请日:
2005.11.10
申请国别(地区):
IS
年份:
2017
代理人:
摘要:
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.
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