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    • 8. 发明专利
    • Preparation of 2,2-dimethyl-5-hydroxythiazolidine derivative
    • 2,2-二甲基-5-羟基噻唑啉衍生物的制备
    • JPS59175478A
    • 1984-10-04
    • JP4876983
    • 1983-03-25
    • Nippon Rikagaku Yakuhin Kk
    • ANDOU WATARUTAMURA YOSHIHARU
    • C07D277/06C07B41/02C07D501/08
    • Y02P20/55
    • PURPOSE: To obtain the titled compound useful as an intermediate for synthesizing caphalosporin, β-lactam antibiotic, by one process simply and easily, by oxidizng a 2,2-dimethylthiazolidine derivative as a raw material with oxygen in the presence of a photosensitizer.
      CONSTITUTION: A 2,2-dimethylthiazolidine derivative shown by the formula I (R
      1 is H, or lower alkyl; R
      2 is amino-protecting group) is oxidized with oxygen in the presence of a photosensitizer in a polar solvent such as methanol, ethanol, acetonitrile, etc. to give a compound shown by the formula II. Preferably Rose Bengale, or methylene blue having good solubility in the polar solvent used in the above-mentioned reaction is used as the photosensitizer. Halogen-, tungsten-, sodium-lamp or mercury vapor lamp is used as a light irradiation lamp. An amount of the photosensitizer added is about 0.5W1wt% based on the raw material compound. The reaction is advanced smoothly by adding DMSO to it.
      COPYRIGHT: (C)1984,JPO&Japio
    • 目的:通过在光敏剂存在下用氧气氧化2,2-二甲基噻唑烷衍生物作为原料,通过简单且容易的方法得到可用作合成头孢菌素β-内酰胺抗生素中间体的标题化合物。 构成:式(I)所示的2,2-二甲基噻唑烷衍生物(R 1是H或低级烷基; R 2是氨基保护基))在极性溶剂中在光敏剂存在下用氧氧化 如甲醇,乙醇,乙腈等,得到式Ⅱ所示的化合物。 优选使用在上述反应中使用的在极性溶剂中具有良好溶解性的玫瑰色孟加拉兰或亚甲蓝作为光敏剂。 卤素灯,钨灯,钠灯或水银灯被用作光照射灯。 加入的光敏剂的量相对于原料化合物为约0.5-1重量%。 通过向其中加入DMSO使反应顺利进行。