Department of Chemistry, ‡Department of Pediatric Dentistry, and §Department of Microbiology, University of Alabama at Birmingham , 901 14th Street South, Birmingham, Alabama 35294, United States.
J Org Chem. 2013 Nov 15;78(22):11525-34. doi: 10.1021/jo402118j. Epub 2013 Nov 5.
Three structurally defined QS-21-based immune adjuvant candidates (2a-2c) have been synthesized. Application of the two-stage activation glycosylation approach utilizing allyl glycoside building blocks improved the synthetic accessibility of the new adjuvants. The efficient synthesis and establishment of the stand-alone adjuvanticity of the examined synthetic adjuvant (2b) open the door to the pursuit of a new series of structurally defined QS-saponin-based synthetic adjuvants.
已经合成了三种结构定义的 QS-21 为基础的免疫佐剂候选物（2a-2c）。利用烯丙基糖苷砌块的两阶段激活糖基化方法的应用提高了新佐剂的合成可及性。所检查的合成佐剂（2b）的高效合成和独立佐剂活性的建立为追求一系列新的结构定义的 QS-皂苷为基础的合成佐剂打开了大门。
