公开(公告)号：US5688948A

公开(公告)日：1997-11-18

申请号：US454567

申请日：1995-05-30

申请人： Kunisuke Izawa ,  Yoshihito Koguchi ,  Hiroshi Shiragami ,  Yumiko Uchida ,  Satoshi Takamatsu

发明人： Kunisuke Izawa ,  Yoshihito Koguchi ,  Hiroshi Shiragami ,  Yumiko Uchida ,  Satoshi Takamatsu

IPC分类号： C07D473/00 ,  C07D473/18 ,  C07H19/16 ,  C07D473/06 ,  C07D473/16 ,  C07D473/30

CPC分类号： C07D473/00 ,  C07D473/18 ,  C07H19/16

摘要： Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar. Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.

摘要翻译： 本文公开了一种用于从核糖核苷合成无环型核苷如阿昔洛韦和更昔洛韦的新颖且工业上有利的方法，该方法包括向核糖核苷如鸟苷和无环糖的酯衍生物的溶液中加入酸催化剂和酸酐， 并加热混合物，由此在核糖核苷的核糖部分和无环糖的酯衍生物之间发生反缩糖反应。 本文还公开了用于分离9-取代嘌呤核苷的工业上有利的方法，其是从核糖核苷合成无环核苷如阿昔洛韦，更昔洛韦等的重要中间体，该方法包括仅将9-异构体从 通过冷却溶液或/和通过向其中加入结晶溶剂而含有9-取代的嘌呤核苷和7-取代的嘌呤核苷的溶液或悬浮液。