摘要
以托品酮为起始原料,与氯甲酸氯乙酯经脱甲基化反应制得脱甲基托品酮(1);1与Boc酸酐反应制得N-Boc-N-去甲托品酮(2);以三仲丁基硼氢化锂为还原剂,2经还原反应立体选择性合成了内型N-Boc-N-去甲托品醇(内型/外型=6.5/1),总收率60%,其结构经1H NMR和ESI-MS确证。
Demethylated tropinone（ 1） was synthesized by reaction of tropinone with 1-chloroethyl chloroformate. N-Boc nortropinone（ 2） was prepared by reaction of 1 with Boc anhydride. 2 was reduced by lithium tri-sec-butylborohydride to achieve endo-N-Boc nortropine stereoselectively（ endo /exo = 6. 5 /1） with an overall yield of 60%. The structure was confirmed by1 H NMR and ESI-MS.
出处
《合成化学》
CAS
CSCD
2015年第10期957-959,共3页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(81460526)
