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    • 4. 发明申请
    • SYNTHETIC INTERMEDIATE OF OXAZOLE COMPOUND AND METHOD FOR PRODUCING THE SAME
    • 奥扎唑化合物的合成中间体及其制备方法
    • WO2011093529A1
    • 2011-08-04
    • PCT/JP2011/052307
    • 2011-01-28
    • OTSUKA PHARMACEUTICAL CO., LTD.YAMAMOTO, AkihiroSHINHAMA, KoichiFUJITA, NobuhisaAKI, ShinjiOGASAWARA, ShinUTSUMI, Naoto
    • YAMAMOTO, AkihiroSHINHAMA, KoichiFUJITA, NobuhisaAKI, ShinjiOGASAWARA, ShinUTSUMI, Naoto
    • C07D211/46C07D405/12C07D498/04
    • C07D211/46C07D405/12C07D498/04
    • An object of the present invention is to provide a method for producing an oxazole compound in a high yield. The object can be achieved by a compound represented by Formula (11): wherein R 1 is a hydrogen atom or lower-alkyl group; R 2 is a 1-piperidyl group substituted at the 4-position with a substituent selected from (A1a) a phenoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1b) a phenoxy-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkyl groups, (A1c) a phenyl-substituted lower-alkoxy lower-alkyl group substituted on the phenyl moiety with halogen, (A1d) a phenyl-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1e) an amino group substituted with a phenyl group substituted with one or more halogen-substituted lower-alkoxy groups, and a lower-alkyl group, and (A1f) a phenyl-substituted lower-alkoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups; n is an integer from 1 to 6; and X 3 is an organic sulfonyloxy group.
    • 本发明的目的是提供以高产率制备恶唑化合物的方法。 该目的可以通过式(11)表示的化合物来实现:其中R1是氢原子或低级烷基; R2是在4-位被取代基取代的1-哌啶基,其具有选自(A1a)在苯基部分被一个或多个卤素取代的低级烷氧基取代的苯氧基的取代基,(A1b)苯氧基取代的低级烷氧基, 在苯基部分被一个或多个卤素取代的低级烷基取代的烷基(A1c)在苯基部分被卤素取代的苯基取代的低级烷氧基低级烷基,(A1d)苯基取代的低级烷基, 在苯基部分被一个或多个卤素取代的低级烷氧基取代的烷基,(A1e)被被一个或多个卤素取代的低级烷氧基取代的苯基取代的氨基和低级烷基, 和(A1f)在苯基部分上被一个或多个卤素取代的低级烷氧基取代的苯基取代的低级烷氧基; n是1至6的整数; X3是有机磺酰氧基。