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    • 3. 发明公开
    • N-CYCLOPROPYL-2-DIFLUOROMETHOXY-3-HALOGENOANILINES AND INTERMEDIATES FOR THE PREPARATION THEREOF
    • N-CYCLOPROPYL-2-DIFLUORMETHOXY-3-HALOGEN-ANILINE UND ZWISCJHENPRODUKTE ZU IHRER HERSTELLUNG
    • EP1031555A4
    • 2002-10-30
    • EP99937023
    • 1999-08-11
    • IHARA CHEMICAL IND CO
    • YOSHIDA YASUOTAKEUCHI HIROAKI
    • C07C205/26C07C205/37C07C217/84C07C229/30C07D215/56
    • C07D215/56C07C205/26C07C205/37C07C217/84C07C229/30C07C2601/02
    • The main tasks of the present invention are to provide, from a raw material which is industrially inexpensive and easy to procure, an N-cyclopropyl-2-difluoromethoxy-3-halogenoaniline which is an important intermediate in production of a quinolonecarboxylic acid having a cyclopropyl group at the 1-position, an isoindolinyl group at the 7-position and a difluoromethoxy group at the 8-position, useful as a synthetic antibacterial agent; and an intermediate used for production thereof. The present invention provides: a difluoromethoxybenzene derivative represented by the following formula (1): wherein X is a halogen atom and Y is a nitro group or an amino group; an N-(1-alkoxycyclopropyl)-2-difluoromethoxy-3-halogenoaniline derivative represented by the following formula (2): wherein X is a halogen atom and R is a lower alkyl group; and an N-cyclopropyl-2-difluoromethoxy-3-halogeno-aniline derivative represented by the following formula (3): wherein X is a halogen atom and R is a hydrogen atom or a 2,2-di(alkoxycarbonyl)ethylene group represented by the following formula (4): -CH=C(CO 2R )2 (wherein R is a lower alkyl group).
    • 本发明的主要任务是从工业上廉价且易于获得的原料中提供N-环丙基-2-二氟甲氧基-3-卤代苯胺,其是生产具有环丙基的喹啉酮羧酸的重要中间体 1-位,7-位的异吲哚啉基和8-位的二氟甲氧基,可用作合成抗菌剂; 和用于其生产的中间体。 本发明提供:由下式(1)表示的二氟甲氧基苯衍生物:其中X为卤素原子,Y为硝基或氨基的 由下式(2)表示的N-(1-烷氧基环丙基)-2-二氟甲氧基-3-卤代苯胺衍生物:其中X是卤素原子,R 1是低级烷基; 和由下式(3)表示的N-环丙基-2-二氟甲氧基-3-卤代苯胺衍生物:其中X是卤素原子,R是氢原子或2,2-二(烷氧基羰基) 由下式(4)表示的亚乙基:-CH = C(CO 2/2)2(其中R 2是低级烷基)。