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纳洛酮盐酸盐经2-甲氧基乙氧基甲基氯(MEMCl)保护,四甲基三乙酰氧硼氢化铵还原得(6?)-3-(甲氧基乙氧基)-甲氧基-17-烯丙基-4,5?-环氧吗啡喃-6,14-二醇,再与1-溴-3,6,9,12,15,18,21-七氧代二十二烷反应后,经对甲苯磺酸脱保护,最后与草酸成盐得纳洛醇醚草酸盐,总收率39%。
Naloxone hydrochloride was protected with 2-methoxyethoxymethyl chloride (MEMCl) and tetramethyl triacetoxyborohydride reduced to give (6?) - 3- (methoxyethoxy) - Methoxy-17-allyl-4,5-epoxy-morphinan-6,14-diol, which was reacted with 1-bromo-3,6,9,12,15,18,21-heptaxo Docosane after the reaction, the p-toluenesulfonic acid deprotection, and finally salicylic acid into naloxol ether oxalate, the total yield of 39%.