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    • 9. 发明专利
    • Production of pyridoxine
    • 吡哆醛的生产
    • JPS59186961A
    • 1984-10-23
    • JP5868283
    • 1983-04-05
    • Dai Ichi Seiyaku Co Ltd
    • SHIMADA SADAKATSUTOUJIYOU TOSHIAKI
    • C07D213/67
    • PURPOSE: To obtain a pyridoxine derivative in high yield without forming by- products under mild conditions, by treating a specific compound with a hard acid and a soft base.
      CONSTITUTION: A compound of formula I (R
      1 and R
      2 are lower alkyl) or a mineral acid salt thereof is mixed with a hard acid and a soft base in molar amounts of about 3 times or more of the compound of formula I or a mineral acid salt thereof if necessary in a solvent, e.g. acetic acid, at room temperature for several hours W several tens of hours under agitation to give a pyridoxine or a mineral acid salt thereof. The hard acid includes AlCl
      3 , AlBr
      3 , boron tribromide or boron tribromide complex salt, etc. having a high positive charge of an electron accepting atom, small size and no easily excitable outer shell electron, and bonding strongly to a base having a great tendency toward bonding to proton, and the soft base includes easily oxidizable ethyl mercaptan, methyl sulfide or NaI, etc. having strongly polarized electron donative atoms, low electronegativity, and capable of associating with vacant orbits of low energy.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:在温和条件下,通过用硬酸和软碱处理特定化合物,可以高产率得到吡哆醇衍生物而不形成副产物。 构成:将式I化合物(R 1和R 2为低级烷基)或其无机酸盐与摩尔量为式I化合物的约3倍或更多的硬酸和软碱混合,或无机酸 其盐如果需要在溶剂中,例如 乙酸,在室温下搅拌数小时数十小时,得到吡哆醇或其无机酸盐。 硬酸包括AlCl 3,AlBr 3,三溴化硼或三溴化硼配合盐等,具有高电荷的电子接受原子,体积小,不易兴奋的外壳电子,并且与具有较大倾向的碱 键合到质子,软碱包括容易氧化的乙硫醇,甲硫醚或NaI等具有强极化的电子给体原子,低电负性,并且能够与低能量的空轨相关联。