【摘要】 为对地西他滨产品中的有关物质进行定量控制,2-脱氧-D-核糖经甲基化及乙酰化反应得到1-O-甲基-2-脱氧-3,5-二-(O-乙酰基)-α,β-呋喃核糖,再与2,4-O,N-双三甲基硅烷基-1,3,5-三嗪(6)发生糖苷化反应后重结晶得到1-[3,5-二-(O-乙酰基)-2-脱氧-α-D-核糖]-5-氮杂胞嘧啶,最后经氨气脱保护得到地西他滨α-型异构体,并经X-单晶衍射确证结构。其中6可由5-氮杂胞嘧啶(5)经六甲基二硅烷胺保护得到。更多还原

【Abstract】 To perform the quality control of decitabine,the α-stereoisomer was synthesized from 2-deoxy-D-ribose by methylation and acetylation to give 1-O-methyl-2-deoxy-3,5-di-(O-acetyl)-α,β-ribofuranose,which was subjected to glycosylation with 2,4-O,N-bis(trimethylsilyl)-1,3,5-triazine(6) followed by deprotection with NH3.Its configuration was confirmed by X-ray.The compound 6 was prepared from 5-azacytosine(5) by protection with hexamethyl disilylamine.更多还原