[EN] PROCESS FOR THE PRODUCTION OF CYCLOPROPANE DERIVATIVES<br/>[FR] PROCÉDÉ DE FABRICATION DE DÉRIVÉS DE CYCLOPROPANE
申请人:DSM FINE CHEM AUSTRIA GMBH
公开号:WO2010055106A1
公开(公告)日:2010-05-20
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 :CR1 R2, in a reaction vessel, optionally in the presence of a solvent, wherein, R1 and R2 are each independently hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, -C(O)R7 or -NR82; R3, R4, R5 and R6 are each independently hydrogen, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, aryl, aryloxy, heteroaryl, heterocyclyl, carbocyclyl, heterocyclyl, -C(O)R9, -NR102, -SR11, -S(O)R11, or -SO2R11, or R3 and R6 are as defined above and R4 and R5 together form a ring, which ring is carbocyclyl, heterocyclyl, aromatic or heteroaromatic; R7 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, aryloxy, heteroaryl or -NR102; R8 is hydrogen, C1-C6 alkyl, C1 -C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; R9 is hydrogen, hydroxy, C1-C6 alkyl, C1 -C6 alkoxy, aryl, aryloxy or heteroaryl; R10 is hydrogen, C1 -C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl, heterocyclyl or C(O)R12; R11 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl, aryl, heteroaryl, carbocyclyl or heterocyclyl; and R12 is hydrogen, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, aryl, or aryloxy, in the presence of copper metal or copper oxide, wherein the process is a continuous process.
一种制备公式(I)的环丙烷衍生物的方法,通过在反应容器中将公式(II)的烯烃与公式:CR1 R2的卡宾反应,可选地在溶剂的存在下进行,其中,R1和R2分别独立地是氢、C1-C6烷基、C2-C6烯基、芳基、杂芳基、杂环烷基、碳环烷基、杂环烷基、-C(O)R7或-NR82;R3、R4、R5和R6分别独立地是氢、C1-C6烷基、C1-C6烷氧基、C2-C6烯基、芳基、芳氧基、杂芳基、杂环烷基、碳环烷基、杂环烷基、-C(O)R9、-NR102、-SR11、-S(O)R11或-SO2R11,或者R3和R6如上所定义,R4和R5一起形成一个环,该环是碳环烷基、杂环烷基、芳香族或杂芳族;R7是氢、羟基、C1-C6烷基、C1-C6烷氧基、芳基、芳氧基、杂芳基或-NR102;R8是氢、C1-C6烷基、C1-C6烯基、芳基、杂芳基、碳环烷基或杂环烷基;R9是氢、羟基、C1-C6烷基、C1-C6烷氧基、芳基、芳氧基或杂芳基;R10是氢、C1-C6烷基、C2-C6烯基、芳基、杂芳基、碳环烷基、杂环烷基或C(O)R12;R11是氢、C1-C6烷基、C2-C6烯基、芳基、杂芳基、碳环烷基或杂环烷基;R12是氢、羟基、C1-C6烷基、C1-C6烷氧基、芳基或芳氧基,在铜金属或氧化铜的存在下进行,其中该过程是一个连续过程。