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    • 5. 发明授权
    • Protecting groups for boronic acids
    • 保护硼酸的基团
    • US09085590B2
    • 2015-07-21
    • US14213433
    • 2014-03-14
    • Wisconsin Alumni Research Foundation
    • Ronald T. RainesBrett VanVellerMatthew Aronoff
    • C07F5/04C07F5/02
    • C07F5/025C07F5/02C07F5/04Y02P20/55
    • Di- and trivalent protecting groups for organoboronic acids including phenyl boronic acids, benzoxaboroles and benzoxaborins, which are prepared from precursor compounds of formula I: where: R1 is a methyl, ethyl or a —(CH2)n—OH group, where n is 2 or 3; R2 and R3 are independently methyl or ethyl groups; R4 and R5 are independently halogens or hydrogens; R6 and R7 are independently hydrogens, halogens, or nitro groups; and R8 and R9 are independently hydrogens, halogens or nitro groups or R8 and R9 together with a portion of the naphthalene ring form a 5-member ring, where when R1 is —CH2—CH2—OH then the protecting group is a trivalent protecting group. Also provided are protected organoboronic acids including protected phenyl boronic acids, benzoxaboroles and benzoxaborins. Also provides are methods for conducting reactions employing protected organoboronic acids.
    • 由式I的前体化合物制备的包括苯基硼酸,苯并恶唑和苯并恶灵素在内的有机硼酸的二价和三价保护基:其中:R1是甲基,乙基或 - (CH2)n-OH基团,其中n是 2或3; R2和R3独立地是甲基或乙基; R4和R5独立地是卤素或氢; R6和R7独立地是氢,卤素或硝基; R8和R9独立地为氢,卤素或硝基,或R8和R9与一部分萘环一起形成5-元环,其中当R1为-CH2-CH2-OH时,则保护基为三价保护基 。 还提供了保护的有机硼酸,包括保护的苯基硼酸,苯并恶唑和苯并恶灵。 还提供了使用保护的有机硼酸进行反应的方法。