一种氯法拉滨及其中间体化合物的制备方法

Preparation method of clolar and intermediate of clolar

Abstract

The invention discloses a preparation method of collar of a formula I, which comprises the step of performing a reaction of a compound VII in alcohol solution of ammonia to remove protective groups R1 and R2 of hydroxyl, wherein R1 is benzoyl and R2 is benzoyl or acetyl; and the alcohol solution of the ammonia is C1 to C4 alkyl alcohol solution of ammonia, which contains 1 to 35 weight percent ofammonia. The invention also discloses a preparation method of the intermediate compound VII of the collar. The preparation methods of the invention has the advantages of short reaction time, high yield, high final product purity, low production cost, simple operation and easy industrial promotion.
本发明公开了一种如式Ⅰ所示的氯法拉滨的制备方法,其包含下列步骤:将化合物Ⅶ在氨的醇溶液中进行脱去羟基的保护基R1和R2的反应,即可;其中,R1为苯甲酰基,R2为苯甲酰基或乙酰基;所述的氨的醇溶液为氨的含量为1~35%(w/w)的C1~C4烷基醇溶液。本发明还公开了氯法拉滨的中间体化合物Ⅶ的制备方法。本发明的制备方法反应时间短,收率高,最终产品纯度高,生产成本低,操作简单,易于产业化推广。

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