摘要
以1-O-乙酰基-2,3,5-三-O-苯甲酰基-β-D-呋喃核糖为原料,经重排获得1,3,5-三-O-苯甲酰基-α-D-呋喃核糖,其与硫酰氯、咪唑反应生成易去基团磺酰咪唑酯,再经氟代、溴化得1-溴-2-氟-3,5-二-O-苯甲酰基-α-D-阿拉伯糖,继而与二氯腺嘌呤缩合后在碱性条件下脱保护基,即可制得抗白血病药氯法拉滨,反应总收率为7.33%。
Clofarabine was synthesized with 1-O-acetyl-2,3,5-trio-O-benzoyl-β-D-ribofuranose as raw material via the six steps of rearrangement, esterification with sulfonated imidazole, fluorination, bromine displacement, condensation with 2-chloroadenine and deprotection, at the total yield of 7.33%.
出处
《药学与临床研究》
2009年第2期107-109,共3页
Pharmaceutical and Clinical Research
关键词
氯法拉滨
抗白血病药
合成
Clofarabine
Antileukemie agent
Synthesis
