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    • 5. 发明公开
    • Preparing clindamycin and analogues thereof
    • Herstellung von Clindamycin und Analoge。
    • EP0161794A2
    • 1985-11-21
    • EP85302494.1
    • 1985-04-09
    • THE UPJOHN COMPANY
    • Livingston, Douglas Alan
    • C07H15/16
    • C07D295/067C07H15/16
    • A process for preparing 7-halo-7-deoxylincomycin or an analogue thereof, which comprises

      (a) reacting a starting compound selected from lincomycin and analogues thereof, with an amide halide having the formula
      wherein each Hal is bromine or chlorine, and either R i and R 2 are independently selected from aryl and C 1-8 alkyl or NR 1 R 2 is morpholino or a heterocyclic ring containing 4 to 8 ring atoms selected from carbon and nitrogen, to form an adduct;
      (b) heating the adduct, to form a 7-halo-7-deoxy adduct; and
      (c) hydrolysing the 7-halo-7-deoxy adduct with an aqueous base.
    • 一种制备7-卤代-7-脱氧霉菌素或其类似物的方法,其包括:(a)使选自林可霉素及其类似物的起始化合物与具有下式的酰胺卤化物反应其中每个Hal为溴 或氯,并且R 1和R 2独立地选自芳基和C 1-8烷基或NR 1 R 2是吗啉代或含有4至8个选自碳和氮的环原子的杂环,以形成加合物;(b)加热加合物 ,以形成7-卤代-7-脱氧加合物; 和(c)用碱水溶液水解7-卤代-7-脱氧加合物。