【摘 要】
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We have recently prepared O-and S-glycosyl aryl boronic acids,which are proved as viable material for further applications.We demonstrate hereby that these compounds are useful in organic synthesis an
【机 构】
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School of Pharmacy,China Pharmaceutical University,24 Tongjiaxiang,Nanjing 210009,P.R.China
【出 处】
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全国药物化学学术会议暨第四届中英药物化学学术会议
论文部分内容阅读
We have recently prepared O-and S-glycosyl aryl boronic acids,which are proved as viable material for further applications.We demonstrate hereby that these compounds are useful in organic synthesis and medicinal chemistry:1)We used S-glycosyl aryl boronic acids for intramolecular aglycon delivery via boron ate complex.Difficult 1,2-cis-O-glycosides could be made from easily available 1,2-trans-S-glycosides through this method with good anomeric specificity.1 2)We then developed a mild aqueous Suzuki-Miyaura coupling under neutral condition,using O-glycosyl aryl boronic acids and iodinated peptides.Yields of the neoglycopeptide products are generally good without racemization of the peptide substrate.2 3)Interestingly,glycosidase inhibiting activity was also revealed on certain O-glycosyl aryl boronic acids.
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