萘呋胺酯草酸盐相关化合物的合成研究

采用四氢糠醇为原料,通过酰化反应得到了对甲基苯磺酸四氢糠醇酯,对甲基苯磺酸四氢糠醇酯与丙二酸二乙酯烷基化反应得到中间体四氢糠基丙二酸二乙酯.在此基础上合成了3-(1-萘基)-2-四氢糠基丙酸、3-(1-萘基)-2-四氢糠基丙酸乙酯、3-(1-萘基)-2-(1-萘甲基)丙酸-N,N-二乙胺基乙酯草酸盐、2-(2-萘甲基)-3-(2-四氢呋喃基)丙酸-N,N-二乙胺基乙酯草酸盐等相关的化合物;两步合成四氢糠基丙二酸二乙酯的产率为77.4%,该方法较已有合成方法产率有较大提高且避免了高压下催化加氢操作,反应更简便,得到的相关化合物达到标准品纯度.

Synthesis Research of Nafronyl Related Compounds

Tetrahydrofurane-2-methanol p-toluenesulfonate was synthesized from tetrahydro-furane-2-methanol by acylation,and diethyl tetrahydrofurfurylmalonate was synthesized by alkylation of tetrahydrofurane-2-methanol p-toluenesulfonate with diethyl malonate, then 3-(1-naphthyl)-2-tetrahydrofuryl propionate, ethyl-3-(1-naphthyl)-2-tetrahydrofurylate, N, N-(diethy1amino)ethyl-3-(1-naphthyl-methyl)-2-tetrahydrofurfuryl propionate, N, N-(diethy1amino)ethyl-3-(2-naphthyl-methyl)-2-tetrahydrofurfuryl propionate were synthesized from diethyl tetrahydrofurfurylmalonate. The yield of diethyl tetrahydrofurfurylmalonate was 77.4%. This method avoids hydrogenating under higher pressure and was feasible with higher yield, also pure standard samples of related compounds were obtained.