9-(β-D-2'-脱氧核糖基)-6-甲基嘌呤的合成  

An Efficient Synthesis of 9-β-D-2'-Deoxyribofuranosyl-6-methylpurine

作　　者：李庶心[1] 江发龙[1] 赵砚瑾[1] 郭金华[1] 王志清[1] 

机构地区：[1]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《有机化学》2006年第10期1394-1397,共4页Chinese Journal of Organic Chemistry

摘　　要：报道了9-(β-D-2'-脱氧核糖基)-6-甲基嘌呤合成的新方法.以肌苷1为原料,经酯化、氯化、氨解得6-氯嘌呤核苷(4),再经过羟基保护、6-位甲基化反应及脱保护反应得到关键中间体6-甲基嘌呤核苷7,用1,3-二氯-1,1,3,3-四异丙基二硅氧烷保护7核糖上的3,5-二羟基,2-羟基与苯氧基硫代甲酰氯反应后得到9,然后与氢化三正丁基锡[HSn(Bu-n)3]还原脱氧,最后脱保护得到目标化合物11.产物结构经MS,1HNMR,元素分析等鉴定.A new method for preparing 9-β-D-2＇-deoxyribofuranosyl-6-methylpurine from inosne （1） is described. Inosne was converted to 6-chlorolpurinenucleoside （4） via esteriflcation, chlorination and deacetylation, then through protecting, deacetylation and deprotecting reactions to give the key intermediate 6-methylpurinenucleoside （7）. The compound 7 was protected with O[Si（i-Pr）2Cl]2 and reacted with phenyl carbonochloridothioate to give compound 9. The compound 9 was converted to target compound 11 by reduction and deprotecting reaction. The structures of these products were identified by MS, 1H NMR spectra and elemental analysis.

关 键 词：核苷 呤核苷 合成 

分 类 号：TQ463.53[化学工程—制药化工]