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以糖精为原料合成二氮杂冠醚和三氮杂冠醚。使糖精与二甘醇或三甘醇二氯化物和N,N-二(β-氯乙基)丁胺的DMF溶液在少量碘化钾存在下烃化、氨解,再用二甘醇或三甘醇的二对甲苯磺酸酯烃化生成保护的冠醚环。后者与20％盐酸作用除去保护基生成游离的环体。此法合成路线短原料价廉易得。二氮杂18-冠-6总产率37％左右。
Synthesis of diaza crown ether and triaza crown ether from saccharin. The saccharin is alkylated with a solution of diethylene glycol or triethylene glycol dichloride and a DMF solution of N, N-bis (β-chloroethyl) butylamine in the presence of a small amount of potassium iodide, aminolysis is carried out, Alkylation of the bis-tosylate of the alcohol to form the protected crown ether ring. The latter with 20% hydrochloric acid to remove the protective group generated free ring. This method is short synthetic route cheap and readily available. Diazepine 18-crown-6 total yield of about 37%.