The 3＇-OH, 4＇-OH and 2＂-OH of kanamycin A were modified in search of new aminoglycosides to overcome resistant enzymes, ANTs and APHs. The key intermediate was a dibenzylidene-protected derivative of kanamycin A. T...The 3＇-OH, 4＇-OH and 2＂-OH of kanamycin A were modified in search of new aminoglycosides to overcome resistant enzymes, ANTs and APHs. The key intermediate was a dibenzylidene-protected derivative of kanamycin A. The aimed sites were masked by benzyl, methyl and allyl groups. Multi-step reactions gave the desired aminoglycoside derivatives but showed less antibiotic activity than kanamycin A.展开更多
Resveratrol-based natural products have received considerable attention as synthetic targets due to their versatile bioactivities and unique structures.Herein,we disclose our efforts toward the syntheses of polynapsti...Resveratrol-based natural products have received considerable attention as synthetic targets due to their versatile bioactivities and unique structures.Herein,we disclose our efforts toward the syntheses of polynapstilbenes A and B,which possess[C8-O-C-C-C7]-type dihydrobenzofuran skeleton that is distinctive compared with the other reported resveratrol-derived natural products.Our approach,featuring an acid-catalyzed conjugate addition followed by cyclization of para-quinone methides and phenols,affords two advanced intermediates that represents the dimethyl-protected aglycon of polynapstilbenes A and B.展开更多
基金National Basic Research Program(973 Program,Grant No.2004CB518904).
文摘The 3＇-OH, 4＇-OH and 2＂-OH of kanamycin A were modified in search of new aminoglycosides to overcome resistant enzymes, ANTs and APHs. The key intermediate was a dibenzylidene-protected derivative of kanamycin A. The aimed sites were masked by benzyl, methyl and allyl groups. Multi-step reactions gave the desired aminoglycoside derivatives but showed less antibiotic activity than kanamycin A.
基金Peking University Health Science Center(Grant No.BMU20130354)State Key Laboratory of Natural and Biomimetic Drugs,and the National Recruitment Program of Global Youth Experts(1000 Plan)
文摘Resveratrol-based natural products have received considerable attention as synthetic targets due to their versatile bioactivities and unique structures.Herein,we disclose our efforts toward the syntheses of polynapstilbenes A and B,which possess[C8-O-C-C-C7]-type dihydrobenzofuran skeleton that is distinctive compared with the other reported resveratrol-derived natural products.Our approach,featuring an acid-catalyzed conjugate addition followed by cyclization of para-quinone methides and phenols,affords two advanced intermediates that represents the dimethyl-protected aglycon of polynapstilbenes A and B.
