摘要
R-四氢罂粟碱与1,5-戊二醇二丙烯酸酯经麦克尔加成反应制得(1R-顺,1'R-顺)-2,2'-(3,11-二氧代-4,10-二氧十三烷亚甲基)二(1,2,3,4,四氢-6,7-二甲氧-2-甲基-1-藜芦基异喹啉(4);4与苯磺酸甲酯经N,N'-双甲基化反应立体选择性地合成了顺苯磺酸阿曲库铵[(1R-trans,1'R-trans)-5],收率67%,含量99%。其结构经1H NMR和13C NMR确证。实验结果表明,N-甲基化反应在最佳反应条件(乙腈为溶剂,于-40℃反应72 h)下,混合物收率78%,(1R-trans,1'R-trans)-5/(1R-cis,1'R-trans)-5/(1R-cis,1'R-cis)-5=70/29/1。
Cisatracurium besylate[（1R-trans,1 ＇R-trans）-5] in the yield of 65% with 99% content was synthesized by Michael addition reaction of R-tetrahydropapaverine base with pentane-1,5-diyldiacrylate,followed by quaternization with methyl benzenesulphonate.The structure was confirmed by 1H NMR and 13C NMR.Under the optimal reaction conditions （acetonitrile as the solvent,at-40 ℃ for 72 h）,the yield of the mixture was 78%,（1R-trans,1 ＇R-trans）-5/（1R-cis,1 ＇R-trans）-5/（1R-cis,1 ＇R-cis）-5 was 70/29/1.
出处
《合成化学》
CAS
CSCD
北大核心
2014年第3期419-422,共4页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(21272163)
