Methods and compounds of production of dipeptidyl peptidase IV inhibitors and intermediates thereof

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专利权人:

ASTRAZENECA AB

发明人:

VU, TRUC CHI,KOLOTUCHIN, SERGEI V.,MAZZULLO, JOHN A.,WANG, JIANJI,WONG, KWOK,YU, JURONG,ZHU, JASON

申请号：

ES12162633

公开号：

ES2526138T3

申请日:

2003.12.04

申请国别(地区):

ES

年份:

2015

代理人:

摘要：

A method of producing a cyclopropyl fused dipeptidyl peptidase IV inhibitor comprising: (a) coupling (αS) -α - [[(1,1-dimethylethoxy) carbonyl] amino] -3-hydroxytricyclo acid [3.3.1.13.7] decane-1-acetic acid or its 1,4-diazabicyclo salt [2.2.2] octane at (1S, 3S, 5S) -2-azabicyclo [3.1.0] hexane-3-carboxamide to produce 3- (aminocarbonyl) - (αS) -α- (3-hydroxytricyclo [3.3.1.1.3.7] dec-1-yl) -α-oxo- (1S, 3S, 5S) -2-azabicyclo acid [3.1.0] hexane-2-ethanecarbamic, 1,1-dimethylethyl ester； (b) dehydrate 3- (aminocarbonyl) - (αS) -α- (3-hydroxytricyclo [3.3.1.13.7] dec-1-yl) -α-oxo- (1S, 3S, 5S) -2- azabicyclo acid [3.1.0] hexane-2-ethanecarbamic, 1,1-dimethyl ethyl ester to produce 3-cyano- (αS) -α- (3- hydroxytricyclo [3.3.1.13.7] dec-1-yl) -ß- oxo- (1S, 3S, 5S) -2-azabicyclo [3.1.0] hexane-2-ethanecarbamic, 1,1-dimethylethyl ester； and (c) deprotecting 3-cyano- (αS) -α- (3-hydroxytricyclo [3.3.1.13.7] dec-1-yl) -α-oxo- (1S, 3S, 5S) -2-azabicice [ 3.1.0] hexane-2-ethanecarbamic, 1,1-dimethyl ethyl ester to form the dipeptidyl peptidase IV inhibitor.Un método para producir un inhibidor de la dipeptidil peptidasa IV a base de pirrolidina fusionada con ciclopropilo, que comprende: (a) acoplar ácido (&alpha；S)-&alpha；-[[(1,1-dimetiletoxi)carbonil]amino]-3-hidroxitriciclo[3.3.1.13,7]decano-1-acético o su sal de 1,4-diazabiciclo[2.2.2]octano a la (1S,3S,5S)-2-azabiciclo[3.1.0]hexano-3-carboxamida para producir ácido 3-(aminocarbonil)-(&alpha；S)-&alpha；-(3-hidroxitriciclo[3.3.1.1.3,7]dec-1-il)-&alpha；-oxo-(1S,3S,5S)-2-azabiciclo[3.1.0]hexano-2- etanocarbámico, 1,1-dimetiletil éster； (b) deshidratar ácido 3-(aminocarbonil)-(&alpha；S)-&alpha；-(3-hidroxitriciclo[3.3.1.13,7]dec-1-il)-&alpha；-oxo-(1S,3S,5S)-2- azabiciclo[3.1.0]hexano-2-etanocarbámico, 1,1-dimetiletil éster para producir ácido 3-ciano-(&alpha；S)-&alpha；-(3- hidroxitriciclo[3.3.1.13,7]dec-1-il)-ß-oxo-(1S,3S,5S)-2-azabiciclo[3.1.0]hexano-2-etanocarbámico, 1,1-dimetiletil éster； y (c) desproteger ácido 3-ciano-(&al

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