氯法拉滨的合成新工艺

New synthetic process of clofarabine

目的:开发一条新的氯法拉滨合成工艺路线,避开已有的专利方法,提高收率与质量。方法:以2-脱氧-2-氟-1,3,5-三苯甲酰基-α-D-阿拉伯呋喃糖(2)为起始原料,经过溴代,与2-氯-6-氨基嘌呤偶联,再经过甲醇解得到氯法拉滨。结果:开发出一种新的偶联方法,产品质量可靠、收率稳定,制备得到的氯法拉滨其结构经MS,1HNMR,13CNMR确证。结论:该合成新方法完全避开已有的专利方法,操作简便,适合于工业化生产。

Objective： To develop a new non-infringing synthetic process of clofarabine. Methods： After bromination,2-deoxy-2-fluoro-1,3,5-tri-O-benzoyl-α-D-ribofuranose（ 2） was reacted with 2,6-dichloropurine to get coupling product,and the clofarabine was obtained after methanolysis of the coupling product. Results： A new coupling method with reliable quality and stable yield was developed,the structure of clofarabine was identified with MS,1HNMR and13 CNMR. Conclusion： The new non-infringing synthetic process is simple and easy to operate,and is suitable for the industrial production.