Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, TN 38163, USA.
Curr Med Chem. 2009;16(20):2531-65. doi: 10.2174/092986709788682010.
Combinatorial chemistry has become an important tool in the area of modern drug discovery and its success is partly dependent on further advances of solid phase organic synthesis (SPOS). Indoles are an important class of compounds with a broad spectrum of biological activities. Therefore, considerable attention is given for the development of effective methodology for the substituted indoles not only in solution phase but also on solid phase. In this review, indole forming classical reactions such as Fisher, Nenitzescu, Bartoli, Modified Madelung, Modified Bischler, and Wittig type reactions on solid support are summarized. In addition, metal mediated cyclizations such as palladium, and rhodium catalyzed cyclizations along with microwave-assisted solid phase synthesis of indoles have been discussed. Also, the most relevant biological properties of indoles have been reported.
组合化学已成为现代药物发现领域的重要工具,其成功在一定程度上取决于固相有机合成(SPOS)的进一步发展。吲哚是一类具有广泛生物活性的重要化合物。因此,人们非常关注发展有效的取代吲哚的方法,不仅在溶液相中,而且在固相上。在这篇综述中,总结了在固相上形成吲哚的经典反应,如 Fisher、Nenitzescu、Bartoli、Modified Madelung、Modified Bischler 和 Wittig 型反应。此外,还讨论了金属介导的环化反应,如钯和铑催化的环化反应以及微波辅助固相合成吲哚。还报告了吲哚的最相关的生物学特性。