阿糖鸟苷与乙酐反应保护糖环上的羟基得2',3',5'-三-O-乙酰基阿糖鸟苷,然后经三氯氧磷氯代得6-氯-2',3',5'-三-O-乙酰基阿糖鸟苷,最后在碳酸钠-甲醇体系中脱除乙酰基,同时用甲氧基取代氯原子制得抗白血病药物奈拉滨,总收率为73%。
Nelarabine, an anti-leukemia drug, was synthesized from guanine arabinoside via condensation with acetic anhydride to give 2',3',5'-tri-O-acetylguanine arabinoside, which was subjected to chlorination with POC13 to obtain 6-chloro-2',3',5'-tri-O-acetylguanine arabinoside, followed by deprotection in the presence of Na2CO3-CH3OH with an overall yield of 73 %.