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2. 发明授权

US5840896A Method of preventing or limiting reperfusion damage 失效
标题翻译：预防或限制再灌注损伤的方法
公开(公告)号：US5840896A
公开(公告)日：1998-11-24
申请号：US424687
申请日：1995-04-18
申请人： Herman Van Belle , Willy Joannes Carolus Van Laerhoven
发明人： Herman Van Belle , Willy Joannes Carolus Van Laerhoven
IPC分类号： A61K31/495 , A61K38/16 , A61K38/49 , C07D241/04
CPC分类号： C07D241/04 , A61K31/495 , A61K38/166 , A61K38/49
摘要： There is disclosed a process for preparing (l)-(-)-2-aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-�5,5-bis(4-fluorophenyl)pentyl!-1-piperazineacetamide which comprises the steps of (a) cyclizing (-)-(S,S)-N.sup.1,N.sup.2 -bis(1-phenylethyl)-1,2-ethanediamine with 2,3-dibromopropanamide in a reaction-inert solvent in the presence of a base, thus yielding an intermediate; (b) resolving the intermediate of into two stereoisomers and recovering thereby �1(S),2A,4(S)!-1,4-bis(1-phenylethyl)-2-piperazinecarboxamide; (c) hydrogenolyzing �1(S),2A,4(S)!-1,4-bis(1-phenylethyl)-2-piperazinecarboxamide under a hydrogen atmosphere in an alkanol in the presence of a hydrogenation catalyst to produce (+) -2-piperazinecarboxamide; (d) reductively N-alkylating (+)-2-piperazinecarboxamide with 5,5-bis(4-fluorophenyl)pentaldehyde under a hydrogen atmosphere in an alkanol in the presence of a hydrogenation catalyst to produce a compound of the formula: ##STR1## (e) N-alkylating the compound of Formula (VII) with an alkylating reagent of the formula: ##STR2## wherein W represents a reactive leaving group, in a reaction-inert solvent in the presence of a base to form the nitro analog of the desired compound; and (f) reducing the nitro compound in the presence of a reducing agent in a reaction-inert solvent.
摘要翻译：公开了制备（1） - （ - ） - 2-氨基羰基）-N-（4-氨基-2,6-二氯苯基）-4- [5,5-双（4-氟苯基）戊基] - 1-（1-苯基乙基）-1,2-乙二胺与2,3-二溴丙酰胺在反应惰性溶剂中环化（ - ） - （S，S）-N1，在碱的存在下，从而产生中间体; （b）将中间体分解成两种立体异构体并由其回收[1（S），2A，4（S）] -1,4-双（1-苯基乙基）-2-哌嗪甲酰胺; （c）在氢气氛下在氢化催化剂存在下，在烷醇中氢解[1（S），2A，4（S）] -1,4-双（1-苯基乙基）-2-哌嗪甲酰胺，生成（+ ）-2-哌嗪甲酰胺; （d）在氢气氛下在氢化催化剂存在下，在链烷醇中还原N-烷基化（+） - 2-哌嗪甲酰胺与5,5-双（4-氟苯基）戊醛，得到下式化合物：

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