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Alkyl esters of polyene antibiotics

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اقرأ أكثر حفظ في قائمتي
  • Publication Date:
    July 26, 1977
  • معلومة اضافية
    • Patent Number:
      4,038,382
    • Appl. No:
      05/630,888
    • Application Filed:
      November 11, 1975
    • نبذة مختصرة :
      The present invention provides a process for the preparation of alkyl esters of polyene antibiotics, wherein a polyene antibiotic is reacted with a diazoalkane in the presence of a basic substance.
      The present invention also provides, as new materials, alkyl esters of polyene antibiotics in which the alkyl radical of the ester grouping contains 2 or more carbon atoms.
    • Inventors:
      Bruzzese, Tiberio (Milan, IT); Ferrari, Rodolfo (Milan, IT)
    • Assignees:
      SPA-Societe Prodotti Antibiotici S.p.A. (IT)
    • Claim:
      We claim
    • Claim:
      1. A process for the preparation of the methyl ester of ayfactin which comprises reacting ayfactin with diazomethane in the presence of a basic substance selected from the group consisting of ammonia, triethylamine and pyridine in a substantially stoichiometric quantity, the resulting pH being 10 to 10.5 (determined after dilution to 1%), the reaction being carried out at a temperature between 15.degree. and 30.degree. C.
    • Claim:
      2. The product of the process of claim 1.
    • Claim:
      3. A process for the preparation of the methyl ester of candicidin which comprises reacting candicidin with diazomethane in the presence of a basic substance selected from the group consisting of ammonia, triethylamine and pyridine in a substantially stoichiometric quantity, the resulting pH being 10 to 10.5 (determined after dilution to 1%), the reaction being carried out at a temperature between 15.degree. and 30.degree. C.
    • Claim:
      4. The product of the process of claim 3.
    • Claim:
      5. A process for the preparation of the methyl ester of nystatin, which comprises reacting nystatin with diazomethane in the presence of a basic substance selected from the group consisting of ammonia, triethylamine and pyridine in a substantially stoichiometric quantity, the resulting pH being 10 to 10.5 (determined after dilution to 1%), the reaction being carried out at a temperature between 15.degree. and 30.degree. C.
    • Claim:
      6. The product of the process of claim 5.
    • Claim:
      7. A process for the preparation of the methyl ester of pimaricin which comprises reacting pimaricin with diazomethane in the presence of a basic substance selected from the group consisting of ammonia, triethylamine and pyridine in a substantially stoichiometric quantity, the resulting pH being 10 to 10.5 (determined after dilution to 1%), the reaction being carried out at a temperature between 15.degree. and 30.degree. C.
    • Claim:
      8. The product of the process of claim 7.
    • Claim:
      9. A process for the preparation of the methyl ester of the heptaene antibiotic DJ-400 which comprises reacting heptaene antibiotic DJ-400 with diazomethane in the presence of a basic substance selected from the group consisting of ammonia, triethylamine and pyridine in a substantially stoichiometric quantity, the resulting pH being 10 to 10.5 (determined after dilution to 1%), the reaction being carried out at a temperature between 15.degree. and 30.degree. C.
    • Claim:
      10. The product of the process of claim 9.
    • Current U.S. Class:
      424/117; 424/115; 424/120; 424/122
    • Current International Class:
      H61K 3500
    • Other References:
      chemical Abstracts 73:35698t and 35699u (1970).
      Chemical Abstracts 80:121291f (1974).
    • Primary Examiner:
      Goldberg, Jerome D.
    • Attorney, Agent or Firm:
      Wenderoth, Lind & Ponack
    • الرقم المعرف:
      edspgr.04038382