2′-对甲苯磺酰基腺苷在醋酸和DMF溶液中用N-氯代琥珀酰亚胺氯化,可得到49％8-氯-2′-对甲苯磺酰基腺苷。后者经环亚磷酰化反应可得到相应的3′,5′-环亚磷酸酯或酰胺,再经氧化或硫化和脱去2′-位保护基得到目标产物。反应中发现3′,5′-环磷酸酯衍生物主要产物是烷氧基处于竖键的异构体,而磷酰胺衍生物则是以胺基处于横键为主要产物。 P-Tosyl adenosine was chlorinated with N-chlorosuccinimide in acetic acid and DMF to give 49% of 8-chloro-2’-p-toluenesulfonyl adenosine. The latter by cyclophosphorylation reaction can be obtained corresponding 3 ’, 5’-cyclic phosphite or amide, and then oxidized or sulfurized and off 2’-position protecting group to obtain the desired product. It was found that the main product of the 3 ’, 5’-cyclophosphate derivative was an isomer with a straight-chain alkoxy group, while the phosphoramide derivative was mainly a product with a lateral bond at the amine group.