摘要
2-脱氧-D核糖在HCl的作用下先经甲氧基化后与对甲基苯甲酰氯进行酰化,再在三氟甲磺酸锂作用下与5-氮杂胞嘧啶偶联得到1-(3,5-二-O-对甲基苯甲酰基-2-脱氧-D核糖)-5-氮杂胞嘧啶,最后经甲醇钠脱保护、甲醇重结晶得抗肿瘤药地西他滨,总收率30.2%。
Decitabine was synthesized from 2-deoxyribose by methoxylation with methanol and then acylation with p-methyl benzoyl chloride,coupling with 5-azacytosine catalyzed by CF3SO3Li to get 1-（3,5-di-O-p-methyl benzoyl-2-deoxy-D-ribofuranosyl）-5-azacytosine,followed by deprotection and recrystallization with an overall yield of about 30.2 %.
出处
《广东化工》
CAS
2013年第15期47-48,共2页
Guangdong Chemical Industry
关键词
地西他滨
抗肿瘤药
合成
decitabine
anticancer drug
synthesis
