摘要
二(3-氨基丙基)乙二胺经对甲苯磺酰化、与1,2-二(对甲苯磺酰氧基)乙烷闭环、90%硫酸脱保护、氢氧化钠碱化制得1,4,8,11-四氮杂环十四烷,再经N1,N4,N8-三保护、与α,α'-二溴对二甲苯桥连、脱保护及成盐制得抗肿瘤药plerixafor,总收率约19%。
Plerixafor was synthesized from bis （3-aminopropyl）ethylene diamine by sulfonylation with p-toluenesulfonyl chloride, cyclization with ethylene bis（p-toluenesulphonate）, deprotection with 90% concentrated sulfuric acid to give 1,4,8,11-tetraazacycloteradecane, which was subjected to protection followed by condensation with α, α＇-dibromo-p-xylene and then deprotection with an overall yield of about 19%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2007年第6期398-400,共3页
Chinese Journal of Pharmaceuticals
基金
国家重点基础研究发展计划(973计划)资助项目(2004CB518908)
