N_1-(芳)烷氧酰基烷酰基-5-氟尿嘧啶的合成  

Synthesis of N_1-(aryl)alkyloxyacyl-5-fluorouracil Derivatives

作　　者：海俐[1] 吴林艳[1] 黄娟[1] 程丽[1] 吴勇[1] 

机构地区：[1]四川大学华西药学院药物化学教研室

出　　处：《四川大学学报（医学版）》2004年第4期552-554,562,共4页Journal of Sichuan University(Medical Sciences)

基　　金：国家自然科学基金 (批准号 3 9970 869)资助

摘　　要：目的　合成有适当脂溶性的 N1 - (芳 )烷氧酰基取代的 5 -氟尿嘧啶衍生物。方法　将 5 -氟尿嘧啶用六甲基二硅烷胺进行硅醚化 ,然后再与不同的二酸单苄酯酰氯反应 ,得目标物 ( ) ;( )经氢化脱苄 ,得目标物 ( ) ;随后与卤代烃发生酯化反应 ,得目标物 ( )。结果　合成了 1 2个 5 -氟尿嘧啶衍生物。结论　合成的 1 2个 5 -氟尿嘧啶衍生物经 1 H- NMR、IR。Objective To synthesize N 1 (aryl)alkyloxyacyl 5 fluorouracil derivatives and investigate their antitumor activities. Methods Title compounds (Ⅰ) were prepared by 5 fluorouracil which was trimethylsilylated by hexamethyl di silazane, and then acylated. Hydrogenization of compounds (Ⅰ) brought on compounds (Ⅱ), which were esterified to produce title compounds (Ⅲ) afterwards. Results Twelve title compounds were synthesized. Conclusion These compounds were designed products confirmed by 1H NMR, IR and MS spectral data.

关 键 词：N1-(芳)烷氧酰基取代的5-氟尿嘧啶衍生物 合成 

分 类 号：R914[医药卫生—药物化学]