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1. 发明授权

US06653472B1 Preparing amidines derived from 6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid 失效
标题翻译：制备衍生自6-羟基-2,5,7,8-四氢苯并二氢吡喃-2-羧酸的脒
公开(公告)号：US06653472B1
公开(公告)日：2003-11-25
申请号：US10070049
申请日：2002-04-26
申请人： Christine Le Breton , Eric Manginot , Jean-Bernard Cazaux
发明人： Christine Le Breton , Eric Manginot , Jean-Bernard Cazaux
IPC分类号： C07D31166
CPC分类号： C07D409/12 , C07D311/66
摘要： New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide wherein A′ is X is —Z1—CO; &rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine; Y is —Z2— or —NR3—Z2, R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4, R4 is alkyl of 1 to 6 carbon atoms; Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms; and R6 is hydrogen or OH.
摘要翻译：用于合成（ - ） - 6-羟基-2,5,7,8-四氢苯并二氢吡喃-2-羧酸的脒衍生物的下述式（II）B的新中间体，例如（S）-N - {4- [4 - [（3,4-二氢-6-羟基-2,5,7,8-四甲基-2H-1-苯并吡喃-2-基） - 羰基] -1-哌嗪基]苯基} 2-噻吩甲酰胺其中A'is X为-Z1-CO; rho为选自哌啶，哌嗪，高哌嗪，2-甲基哌嗪，2,5-二甲基哌嗪和4-氨基哌啶的键或杂环; Y为 - Z2-或-NR3-Z2，R3是氢，1至6个碳原子的烷基或-COR4，R4是1至6个碳原子的烷基; Z1和Z2独立地是单键或1至6个碳原子的亚烷基; 并且R 6是氢或OH。

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