【摘要】：目的:開發(fā)一條新的氯法拉濱合成工藝路線,避開已有的專利方法,提高收率與質(zhì)量。方法:以2-脫氧-2-氟-1,3,5-三苯甲�；�-α-D-阿拉伯呋喃糖(2)為起始原料,經(jīng)過溴代,與2-氯-6-氨基嘌呤偶聯(lián),再經(jīng)過甲醇解得到氯法拉濱。結(jié)果:開發(fā)出一種新的偶聯(lián)方法,產(chǎn)品質(zhì)量可靠、收率穩(wěn)定,制備得到的氯法拉濱其結(jié)構(gòu)經(jīng)MS,1HNMR,13CNMR確證。結(jié)論:該合成新方法完全避開已有的專利方法,操作簡便,適合于工業(yè)化生產(chǎn)。
[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-偽-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.
【作者單位】： 武漢百科藥物開發(fā)有限公司;武漢海特生物制藥股份有限公司;
【分類號(hào)】：R914.5
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本文編號(hào)：2443532