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    • 3. 发明授权
    • Process for the production of cyclopropane derivatives
    • 制备环丙烷衍生物的方法
    • US08497384B2
    • 2013-07-30
    • US13129213
    • 2009-11-12
    • Mehul ThathagarPeter PoechlauerSascha Braune
    • Mehul ThathagarPeter PoechlauerSascha Braune
    • C07D333/78
    • 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:CR1R2, 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.
    • 一种制备式(I)的环丙烷衍生物的方法,通过使式(II)的烯烃与式CR1R2的卡宾反应在反应容器中,任选地在溶剂存在下,其中R 1 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 82; R3,R4,R5和R6各自独立地为氢,C1-C6烷基,C1-C6烷氧基,C2-C6烯基,芳基,芳氧基,杂芳基,杂环基,碳环基,杂环基,-C(O)R9,-NR102, SR11,-S(O)R11或-SO2R11,或R3和R6如上定义,R4和R5一起形成环,该环是碳环基,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 102; R 8是氢,C 1 -C 6烷基,C 1 -C 6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。
    • 7. 发明申请
    • PROCESS FOR THE PRODUCTION OF CYCLOPROPANE DERIVATIVES
    • 生产环丙基衍生物的方法
    • US20110301359A1
    • 2011-12-08
    • US13129213
    • 2009-11-12
    • Mehul ThathagarPeter PoechlauerSascha Braune
    • Mehul ThathagarPeter PoechlauerSascha Braune
    • C07D333/78
    • 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: CR1R2, 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.
    • 一种制备式(I)的环丙烷衍生物的方法,通过使式(II)的烯烃与式CR1R2的卡宾反应在反应容器中,任选地在溶剂存在下,其中R 1 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 82; R3,R4,R5和R6各自独立地为氢,C1-C6烷基,C1-C6烷氧基,C2-C6烯基,芳基,芳氧基,杂芳基,杂环基,碳环基,杂环基,-C(O)R9,-NR102, SR11,-S(O)R11或-SO2R11,或R3和R6如上定义,R4和R5一起形成环,该环是碳环基,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 102; R 8是氢,C 1 -C 6烷基,C 1 -C 6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。
    • 10. 发明授权
    • Preparation of aromatic and heteroaromatic carboxylic acids by catalytic ozonolysis
    • 通过催化臭氧分解制备芳香族和杂芳族羧酸
    • US07371866B2
    • 2008-05-13
    • US10437994
    • 2003-05-15
    • Walther JaryPeter PoechlauerThorsten Ganglberger
    • Walther JaryPeter PoechlauerThorsten Ganglberger
    • C07D213/80C07D213/803C07D213/807C07C51/265
    • C07D213/803C07C51/34C07D213/55C07C63/04C07C63/70
    • A process for catalytically oxidizing alkylaromatic compounds of the formula (I) Ar—CH2—R where Ar is an optionally substituted, aromatic or heteroaromatic 5-membered or 6-membered ring or a ring system having up to 20 carbon atoms where Ar may optionally be fused to a C1-C6-alkyl group in which up to 2 carbon atoms may be replaced by a heteroatom, and R is hydrogen, phenyl, benzyl or heteroaryl, where the phenyl, benzyl or heteroaryl radicals may also be joined to Ar by a bridge, or R together with Ar forms an optionally substituted ring system which may contain one or more optionally substituted heteroatoms, to the corresponding aromatic or heteroaromatic carboxylic acids in a solvent with ozone in the presence of a transition metal catalyst and optionally in the presence of an acid at a temperature between −70° C. and 110° C. to the corresponding carboxylic acid.
    • 用于催化氧化式(I)的烷基芳族化合物的方法<?in-line-formula description =“In-line Formulas”end =“lead”→Ar-CH 2 -R < 在线公式描述=“在线公式”end =“tail”?>其中Ar是任选取代的芳族或杂芳族5元或6元环或具有至多20个碳原子的环系,其中Ar 可以任选地与C 1 -C 6 - C 6 - 烷基稠合,其中最多2个碳原子可以被杂原子代替,并且R是氢,苯基,苄基 或杂芳基,其中苯基,苄基或杂芳基也可以通过桥连接到Ar,或者R与Ar一起形成可以含有一个或多个任选取代的杂原子的任选取代的环系统到相应的芳族或杂芳族羧酸 在含有过渡金属催化剂的臭氧的溶剂中,任选在酸存在下,在-70℃至110℃的温度下进行。 到相应的羧酸。