氯法拉滨的合成新工艺
发布时间：2019-03-19 12:42
【摘要】：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。
[Abstract]:Aim: to develop a new synthetic route of chlorfarabine, avoid the existing patent method, and improve the yield and quality. Methods: chlorfarabine was synthesized from 2-deoxy-2-fluoro-1,3,5-tribenzoyl-伪-D-arabinose (2) by bromination, coupling with 2-chloro-6-aminopurinine and methanol hydrolysis. Results: a new coupling method was developed. The quality of the product was reliable and the yield was stable. The structure of the prepared chlorfarabine was confirmed by MS,1HNMR,13CNMR. Conclusion: the new synthesis method avoids the patent method completely and is easy to operate. It is suitable for industrial production.
【作者单位】： 武汉百科药物开发有限公司;武汉海特生物制药股份有限公司;
【分类号】：R914.5
，
本文编号：2443532
[Abstract]:Aim: to develop a new synthetic route of chlorfarabine, avoid the existing patent method, and improve the yield and quality. Methods: chlorfarabine was synthesized from 2-deoxy-2-fluoro-1,3,5-tribenzoyl-伪-D-arabinose (2) by bromination, coupling with 2-chloro-6-aminopurinine and methanol hydrolysis. Results: a new coupling method was developed. The quality of the product was reliable and the yield was stable. The structure of the prepared chlorfarabine was confirmed by MS,1HNMR,13CNMR. Conclusion: the new synthesis method avoids the patent method completely and is easy to operate. It is suitable for industrial production.
【作者单位】： 武汉百科药物开发有限公司;武汉海特生物制药股份有限公司;
【分类号】：R914.5
，
本文编号：2443532
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