普乐沙福的合成工艺改进  

Process Improvement on the Synthesis of Plerixafor

作　　者：陈贝贝[1] 强斌[1] 卓广澜[1] 

机构地区：[1]浙江理工大学化学系,浙江杭州310018

出　　处：《合成化学》2015年第8期774-777,共4页Chinese Journal of Synthetic Chemistry

摘　　要：以二(3-氨基丙基)乙二胺为起始原料,经对甲苯磺酰化、与1,2-二(对甲苯磺酰氧基)乙烷闭环、硫酸脱保护、氢氧化钠碱化制得1,4,8,11-四氮杂环十四烷(5);5经N1,N4,N8-三保护、与α,α-二溴对二甲苯桥连和脱保反应合成了抗肿瘤药普乐沙福,总收率30%,其结构经1H NMR和ESI-MS确证。The key intermediate, 1,4,8,11 -tetraazacycloteradecane （5）, was preapred by sulfonyla- tion with p-toluenesulfonyl chloride, cyclization with ethylene bis（p-toluenesulphonate）, deprotection with concentrated sulfuric acid using bis （3-aminopropyl）ethylene diamine as the starting material. Plerixafor was synthesized by protection, condensation with α, α-dibromo-p-xylene and then deprotec- tion from 5, the overall yield was 30%. The structure was confirmed by 1H NMR and ESI-MS.

关 键 词：二(3-氨基丙基)乙二胺 普乐沙福 抗肿瘤药 合成 工艺改进 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]