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PROCESS FOR THE PREPARATION OF N-SUBSTITUTED 2-CYANOPYRROLIDINES
专利权人:
NOVARTIS AG
发明人:
SCHAFER FRANK,SCHAFER Frank,SEDELMEIER GOTTFRIED,SEDELMEIER Gottfried
申请号:
SI200432220
公开号:
SI1620396T1
申请日:
2004.04.15
申请国别(地区):
SI
年份:
2015
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, X1 and X3 are halogen X2 is halogen, OH, O-C(-O)-CH2X3, -O-SO2-(C1-8)alkyl or 13 O-SO2-(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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