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    • 1. 发明申请
    • PROCESS FOR THE PRODUCTION OF CYCLOPROPANE DERIVATIVES
    • 生产环丙基衍生物的方法
    • WO2010055106A1
    • 2010-05-20
    • PCT/EP2009/065075
    • 2009-11-12
    • DSM FINE CHEMICALS AUSTRIA NFG. GMBH & CO KGTHATHAGAR, MehulPOECHLAUER, PeterBRAUNE, Sascha
    • THATHAGAR, MehulPOECHLAUER, PeterBRAUNE, Sascha
    • C07B37/10C07B61/00C07D333/78
    • C07B37/10C07D333/78Y02P20/582
    • A process for the preparation of a cyclopropane derivative of Formula (I), by reacting an olefin of Formula (II), with a carbene of the formula :CR 1 R 2 , in a reaction vessel, optionally in the presence of a solvent, wherein, R 1 and R 2 are each independently hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, -C(O)R 7 or -NR 8 2 ; R 3 , R 4 , R 5 and R 6 are each independently hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, -C(O)R 9 , -NR 10 2, -SR 11 , -S(O)R 11 , or -SO 2 R 11 , or R 3 and R 6 are as defined above and R 4 and R 5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R 7 is hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, aryl, aryloxy, heteroaryl or -NR 10 2 ; R 8 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R 9 is hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, aryl, aryloxy or heteroaryl; R 10 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, heteroaryl, carbocyclyl, heterocyclyl or C(O)R 12 ; R 11 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; and R 12 is hydrogen, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, aryl, or aryloxy, in the presence of copper metal or copper oxide, wherein the process is a continuous process.
    • 任选地在溶剂存在下,通过使式(II)的烯烃与式CR1R2的卡宾反应,在反应容器中制备式(I)的环丙烷衍生物的方法,其中, R 1和R 2各自独立地为氢,C 1 -C 6烷基,C 2 -C 6烯基,芳基,杂芳基,杂环基,碳环基,杂环基,-C(O)R 7或-NR 8 2; R 3,R 4,R 5和R 6各自独立地为氢,C 1 -C 6烷基,C 1 -C 6烷氧基,C 2 -C 6烯基,芳基,芳氧基,杂芳基,杂环基,碳环基,杂环基,-C(O) -SR 11,-S(O)R 11或-SO 2 R 11,或R 3和R 6如上所定义,并且R 4和R 5一起形成环,该环为碳环基,杂环基,芳族或杂芳族; R 7是氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,芳基,芳氧基,杂芳基或-NR 10 2; R 8是氢,C 1 -C 6烷基,C 1 -C 6链烯基,芳基,杂芳基,碳环基或杂环基; R9是氢,羟基,C1-C6烷基,C1-C6烷氧基,芳基,芳氧基或杂芳基; R 10是氢,C 1 -C 6烷基,C 2 -C 6烯基,芳基,杂芳基,碳环基,杂环基或C(O)R 12; R11是氢,C1-C6烷基,C2-C6烯基,芳基,杂芳基,碳环基或杂环基; 并且在铜金属或氧化铜的存在下,R 12是氢,羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,芳基或芳氧基,其中该方法是连续方法。