公开(公告)号：US20050165078A1

公开(公告)日：2005-07-28

申请号：US10510439

申请日：2003-04-08

申请人： Hansgeorg Ernst ,  Jurgen Koppenhofer ,  Daniela Klein

发明人： Hansgeorg Ernst ,  Jurgen Koppenhofer ,  Daniela Klein

IPC分类号： C07D233/34 ,  C07B53/00 ,  C07B61/00 ,  C07D233/00 ,  A61K31/4178 ,  A61K31/4168 ,  C07D233/04 ,  C07D47/02

CPC分类号： C07D233/00

摘要： The invention relates to a process for preparing chiral imidazolidin-2-ones of the formula I in which R1 is C1-C8-alkyl, cyclohexyl, phenyl, a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, C1-C6-alkylmercapto- or CF3-substituted phenyl radical, naphthyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy- or CF3-substituted naphthyl radical, R2 is C1-C8-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a phenyl-C1-C6-alkyl radical which may be substituted by a nitro, C1-C6-alkoxy, methylenedioxy or CF3 radical, and R3 is C1-C12-alkyl, C2-C8-alkenyl, cyclohexyl, phenyl or a C1-C6-alkyl-, halo-, nitro-, C1-C6-alkoxy-, methylenedioxy-, dialkylamino- or CF3-substituted phenyl radical, by reacting a compound of the formula II or the salt thereof in which R1, R2 and R3 have the abovementioned meaning, with urea in the presence of an involatile ammonium salt, wherein the reaction is carried out in the presence of an aprotic polar organic solvent.

摘要翻译： 本发明涉及一种制备其中R 1是C 1 -C 8 - 的式I的手性咪唑烷-2-酮的方法， 烷基，环己基，苯基，C 1 -C 6 - 烷基 - ，卤代 - ，硝基 - ，C 1 -C 3 - C 6 - 烷氧基 - ，C 1 -C 6 - 烷基巯基或CF 3 - 取代的苯基，萘基或C C 1 -C 6 - 烷基 - ，卤代 - ，硝基 - ，C 1 -C 6 - 烷氧基 - 或CF 3 - 取代的萘基，R 2是C 1 -C 8 - 烷基，C _{和R 3具有上述含义，在非挥发性铵盐存在下用脲进行反应，其中反应在非质子极性有机溶剂的存在下进行。}