A novel fluorous polystyrene (FPS) MR-resin was applied to a fluorous solid-phase (FSP) reaction. The MR-FPS resin actually was developed previously and possessed excellent chemical resistance to acids and alkalis, and a fluorous-tagged compound was homogeneously and loosely immobilized on the resin. The synthesis of an antitumor drug, an N-methyl-N-nirosourea conjugated 3-amino-β-carboline derivative, was accomplished with a high yield by using this new fluorous reaction system. Using only filtration, the fluorous 3-amino-β-carboline derivatives immobilized on the MR-FPS resin were easily recovered from the reaction mixtures. As an extention of this approach, a diversity synthesis of 3-amino-9-benzyl-β-carboline derivatives was applied to the FSP method giving high yields. Finally, the FSP synthesis was compared with the corresponding conventional solid- and liquid-phase methods of synthesis. The FSP reaction was superior in terms of the reactivity of the substrate and the ease of product separation.

中文翻译：

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新型大网状氟聚苯乙烯树脂及其在氟固相反应与N-甲基-N-亚硝基脲共轭合成3-氨基-β-咔啉衍生物中的应用：氟固，固，氟的比较研究， 和

新型氟聚苯乙烯（FPS）MR树脂应用于氟固相（FSP）反应。MR-FPS树脂实际上是以前开发的，对酸和碱具有优异的耐化学性，并且将含氟标签的化合物均匀且松散地固定在树脂上。通过使用这种新型的荧光反应系统，可以高收率地合成抗肿瘤药物，即N-甲基-N-尼罗脲共轭的3-氨基-β-咔啉衍生物。仅使用过滤，就容易从反应混合物中回收固定在MR-FPS树脂上的氟代3-氨基-β-咔啉衍生物。作为该方法的扩展，将3-氨基-9-苄基-β-咔啉衍生物的多样性合成应用于FSP方法，从而获得了高收率。最后，将FSP合成与相应的常规固相和液相合成方法进行了比较。就底物的反应性和产物分离的容易性而言，FSP反应是优异的。