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纳络酮是吗啡类药物中毒的特效解毒剂,也是研究脑神经介质功能的重要工具药物。一般是采用蒂巴因为原料,经氧化,还原制成14-羟基7,8-二氢可待因酮Ⅰ后,与盐酸吡啶或三溴化硼反应将3-位甲醚基的甲基裂去,制成14-羟基7,8-二氢吗啡酮Ⅱ,经酰化制得Ⅲ,氰化制成Ⅳ,水解制成14-羟基7,8-二氢降吗啡酮Ⅴ,再经烯丙基化制成纳络酮Ⅵ。由于(Ⅰ)具有3-甲氧基和氧环两个醚基,在制备Ⅱ时采用选择性较高的试剂三溴化硼收率较
Naloxone is a specific antidote to morphine poisoning and an important tool to study the function of brain nerve mediators. The general is the use of raw materials because of Tiba, after oxidation, reduction made of 14-hydroxy 7,8-dihydrocodein I, with pyridine hydrochloride or boron tribromide reaction 3-methyl ether methyl split To make 14-hydroxy 7,8-dihydromorphorin II, the acylation obtained III, cyanide made of Ⅳ, hydrolyzed to 14-hydroxy 7,8-dihydroporpholin-V, then ene Naloxone VI was made by propylation. Since (I) has two ether groups of 3-methoxy and 2-oxo, the selectivity to boron tribromide is higher when preparing II