报道了抗白血病药物克拉屈滨的合成新方法：在NaH作用下，廉价易得的6-氯嘌呤高选择性地在β位和1-氯-2-脱氧-3，5-二-O-对氯苯甲酰基-D-核糖缩合；β-缩合物的2位在三氟乙酸酐和四丁基硝酸铵作用下引入硝基；在NH4 Cl／EtOH作用下，2-硝基转化为2-氯；最后在饱和NH3／CH3 OH溶液中完成保护基脱除和6-氯氨解两步反应，以4步共43.5％的总收率得到抗白血病药物克拉屈滨。该方法完全避免了α异构体的生成，原料廉价易得，分离纯化不需柱层析，且反应扩大到100 g规模时，收率无下降，具有较好的应用前景。
Cladribine, an anti-leukemia drug, was synthesized in 43.5% total yield by 4 steps.Readily available 6-chloropurine was glycosylated with 1-chloro-3 ,5-di-O-p-benzoyl-D-ribose with good selectivity for βanomer in the presence of NaH .The C2-H ofβ-glycosylated product was converted into C 2-NO2 using 2,2,2-trifluoroacetic anhydride and tetrabutylammonium nitrate , followed by the transformation of C 2-NO2 into C2-Cl in NH4 Cl/EtOH solution . The deprotection step and ammonolysis of C 6-Cl were accomplished in NH3/CH3 OH.The separation ofα-anomer, expensive starting materials and chromatography are not required. Moreover , cladribine could be produced on a 100 gram scale with maintained yield , indicating good potential in industrial applications .
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