CAJ | 학술논문

目的发展一种新的选择性环氨基甲酸酯保护策略,用以合成具有环氨基甲酸酯结构的新型核糖霉素衍生物.方法全苄氨羰基保护的核糖霉素在氢化钠作用下环合,通过控制反应条件选择性在不同位点引入环状氨基甲酸酯保护基.将苄氧羰基催化氢化脱除可得含有环氨基甲酸酯结构的核糖霉素衍生物.结果通过反应条件的控制成功地实现了核糖霉素的选择性环氨基甲酸酯保护.脱保护得到了的核糖霉素衍生物,但并没有预期的抗菌活性. 结论含有环氨基甲酸酯的核糖霉素衍生物的合成表明选择性环氨基甲酸酯保护策略是方便可行的.具有环氨基甲酸酯结构的核糖霉素衍生物可能并不具有抗菌活性.
목적 발전일충신적선택성배안기갑산지보호책략,용이합성구유배안기갑산지결구적신형핵당매소연생물.방법 전변안탄기보호적핵당매소재경화납작용하배합,통과공제반응조건선택성재불동위점인입배상안기갑산지보호기.장변양탄기최화경화탈제가득함유배안기갑산지결구적핵당매소연생물.결과 통과반응조건적공제성공지실현료핵당매소적선택성배안기갑산지보호.탈보호득도료적핵당매소연생물,단병몰유예기적항균활성. 결론함유배안기갑산지적핵당매소연생물적합성표명선택성배안기갑산지보호책략시방편가행적.구유배안기갑산지결구적핵당매소연생물가능병불구유항균활성.
Aim To develop a novel selective protection strategy tor the synthesis ot nbostamycm cyclic carbamate derivatives.Methods Ribostamycin protected by carbobenzoxy group was treated with NaH,to give different protected intermediates under respective controllable cyclization reaction conditioas.New ribostamycin derivative was obtained after the cleavage of carbobenzoxy groups.Result The novel selective protection of ribostamycin was achieved by the synthesis of protected intermediates.New ribostamycin derivative was obtained.but showed no expected antibacterial activity.Conclusion Several ribostamycin cyclic carbamate derivatives were obtained by hovel selective protection strategy,which shows the practicability and convenience of the protection strategy.But these new ribostamycin derivatives containing cyclic carbamates structure may not be an ideal leading compound for antibiotic activity.