Meyers H V, Dilley G J, Durgin T L, Powers T S, Winssinger N A, Zhu H, Pavia M R
Sphinx Pharmaceuticals, Division of Eli Lilly & Co., Cambridge, MA 02139, USA.
Mol Divers. 1995 Sep;1(1):13-20. doi: 10.1007/BF01715805.
A series of analogous arrays of small, non-peptidyl, non-oligomeric compounds were synthesized on polystyrene resin. With the aid of a functionally differentiated phenolic scaffold, the batch preparation of unique benzamide and urea resins was accomplished, which were further derivatized in modified 96-well plates. An efficient cleavage reaction of the phenyl benzoate link enabled the isolation of more than 600 phenolic compounds in milligram quantities that were suitable for direct biological screening. The technology described herein represents a facile, economical approach to non-peptidyl chemical diversity.
一系列类似的小分子、非肽基、非寡聚化合物阵列在聚苯乙烯树脂上合成。借助功能分化的酚类支架,完成了独特的苯甲酰胺和尿素树脂的批量制备,并在改良的96孔板中进一步衍生化。苯甲酸苯酯连接的有效裂解反应能够以毫克量分离出600多种适合直接进行生物筛选的酚类化合物。本文所述技术代表了一种简便、经济的非肽基化学多样性方法。