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氯法拉滨及其α异构体的合成

Pharmaceutical Journal of Chinese People's Liberation Army(2012)

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Abstract
目的优化合成氯法拉滨及其α异构体的合成路线。方法以2-脱氧-2-β-氟-1,3,5-三-氧-苯甲酰基-α-D-呋喃核糖经溴化反应,再与2-氯腺嘌呤在叔丁醇钾作用下缩合后,碱性条件下脱去糖基保护基制得氯法拉滨(1)和氯法拉滨α异构体(6)。结果总收率为28%,目标化合物的结构经IR、1HNMR、13CNMR、MS等方法确证。结论该合成工艺具有操作简便、产率较高、易于工业化生产等特点。
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Key words
cloferabine α-isomer,cloferabine,synthesis
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