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公开(公告)号：EP1896411A2
公开(公告)日：2008-03-12
申请号：EP06754143.3
申请日：2006-06-06
申请人： Novartis AG
发明人： MICKEL, Stuart, John , SEDELMEIER, Gottfried , HIRT, Hans , SCHÄFER, Frank , FOULKES, Michael , PRIKOSZOVICH, Walter
IPC分类号： C07D207/08 , C07D207/16 , C07D407/04
CPC分类号： C07D405/04 , C07C237/22 , C07D207/08 , C07D307/32 , C07D307/33 , Y02P20/55
摘要： The invention related to a novel process, novel process Steps and novel intermediates useful in the synthesis of pharmaceutically active Compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a Compound of the formula (III), wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof, said manufacture comprising (preferably consisting in) reacting a Compound of the formula (I) with a reagent able to transform hydroxy into X where X is for example a leaving group.
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2.发明公开
公开(公告)号：EP1620396A1
公开(公告)日：2006-02-01
申请号：EP04727557.3
申请日：2004-04-15
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： C07D207/16 , A61K31/401 , A61P3/10
CPC分类号： C07D207/16
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 -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 cornpound in free form or in acid addition salt form.
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3.发明授权
公开(公告)号：EP1620396B1
公开(公告)日：2014-12-03
申请号：EP04727557.3
申请日：2004-04-15
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： C07D207/16 , A61K31/401 , A61P3/10
CPC分类号： C07D207/16
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