刘懋勤, 迟传金, 朱淬砺. 纳络酮合成法的改良J. 药学学报, 1982, 17(7): 546-548.
引用本文: 刘懋勤, 迟传金, 朱淬砺. 纳络酮合成法的改良J. 药学学报, 1982, 17(7): 546-548.
LIU Mao-qin, CHI Chuan-jin , ZHU Cui-li (Chu Sae-lee), . AN IMPROVED METHOD FOR THE SYNTHESIS OF NALOXONEJ. Acta Pharmaceutica Sinica, 1982, 17(7): 546-548.
Citation: LIU Mao-qin, CHI Chuan-jin , ZHU Cui-li (Chu Sae-lee), . AN IMPROVED METHOD FOR THE SYNTHESIS OF NALOXONEJ. Acta Pharmaceutica Sinica, 1982, 17(7): 546-548.

纳络酮合成法的改良

AN IMPROVED METHOD FOR THE SYNTHESIS OF NALOXONE

  • Abstract: A new efficient route for the synthesis of naloxone is reported. Acetylation of 14-hydroxy-7,8-dihydrocodeinone with acetic anhydride and treatment of the resulting 14-acetoxy compound with cyanogen bromide gave 17-cyano derivative. Thelatter compound reacted with boron tribromide in chloroform yielding 14-acetoxy-17-cyano-7,8-dihydro-normorphinone, which after hydrolysis led to 14-hydroxy-7,8-dihydronormorphinone. N-allylation of the Secondary amine gave naloxone. The total yield was 53.3%. It appears that this method is better than those reported in the literature because of higher yield and simpler operation.

     

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