5'-脱氧-5-氟-N-[(戊氧基)羰基]胞苷-2',3'-二乙酸酯的合成改进  

Synthesis of 5'-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl] cytidine 2',3'-diacetate

作　　者：陈言德[1] 王志贤[1] 谢斌[1] 韩立[1] 

机构地区：[1]江苏(泰州)新药研究院扬子江药业集团有限公司,江苏泰州225321

出　　处：《精细化工中间体》2010年第6期37-38,42,共3页Fine Chemical Intermediates

摘　　要：5'-脱氧-5-氟-N-[(戊氧基)羰基]胞苷-2',3'-二乙酸酯是合成卡培他滨的关键中间体,它是由1,2,3-三-O-乙酰基-5-脱氧-D-核糖与用三甲基硅烷保护的5-氟胞嘧啶进行缩合反应得中间体5-脱氧-2,3-二-D-乙酰基-5-氟胞苷,再与氯甲酸正戊酯进行酰胺化制得。总收率约70%。5'-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine 2',3'-diacetate,which is a key intermediate of capecitabine,was prepared from the reaction of 1,2,3-O-triacetyl-5-deoxy-D-ribose and trimethylsilyl protected 5-fluorocytosine,followed by reaction with n-amyl chloroformate,in an overall yield of 70%.

关 键 词：合成 卡培他滨 l 2 3-三-O-乙酰基-5-脱氧-D-核糖 氯甲酸正戊酯 

分 类 号：R914[医药卫生—药物化学]