公开(公告)号：US07268228B2

公开(公告)日：2007-09-11

申请号：US10344225

申请日：2001-08-10

申请人： Won Koo Lee ,  Chan Sun Park ,  Yeon Hwa Lim ,  Hyun J on Ha

发明人： Won Koo Lee ,  Chan Sun Park ,  Yeon Hwa Lim ,  Hyun J on Ha

IPC分类号： C07D251/16 ,  C07D203/16 ,  C07D203/04

CPC分类号： C07D203/08

摘要： This invention relates to compounds of Formula I having an aziridine-2-carboxylic group and a menthol group, a process for preparing such compounds, a method for obtaining optically active aziridine-2-carboxylate derivatives by optical resolution of such compounds, and optically active aziridine-2-carboxylate derivatives obtained by the same method: wherein R1 is hydrogen; alkyl; cycloalkyl; 4-chlorophenyl; 4-methoxyphenyl; s-triazinyl or pyridinyl acyl; benzyl; hydrocarbon residue which may be substituted with a substituent selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl and 4-methoxyphenyl; 2,4-dimethoxyphenyl; substituted phenyl including (1R)-phenylethyl or (1S)-phenylethyl. Preferences are given to (1R)-phenylethyl and (1S)-phenylethyl. Menthol is selected from the group consisting of (+)-menthol and (−)-menthol.

摘要翻译： 本发明涉及具有氮丙啶-2-羧酸基和薄荷醇基团的式I化合物，制备这些化合物的方法，通过这种化合物的光学拆分获得光学活性氮丙啶-2-羧酸酯衍生物的方法和光学活性 通过相同方法得到的氮丙啶-2-羧酸酯衍生物：其中R 1是氢; 烷基; 环烷基 4-氯苯基; 4-甲氧基苯基; s-三嗪基或吡啶基酰基; 苄基; 可以被选自羟基，烷氧基，二烷基氨基，苯基，4-氯苯基和4-甲氧基苯基的取代基取代的烃残基; 2,4-二甲氧基苯基; 包括（1R） - 苯基乙基或（1S） - 苯基乙基的取代的苯基。 给予（1R） - 苯基乙基和（1S） - 苯基乙基。 薄荷醇选自（+） - 薄荷醇和（ - ） - 薄荷醇组成的组。