Dubrovskiy Anton V, Markina Nataliya A, Larock Richard C
Department of Chemistry, Iowa State University, Ames, IA 50011, USA.
Comb Chem High Throughput Screen. 2012 Jul;15(6):451-72. doi: 10.2174/138620712800563927.
The iodocyclization of functionally-substituted alkynes provides an excellent way to prepare a wide range of iodoheterocycles, which can then be readily elaborated through palladium-catalyzed Suzuki-Miyaura, Sonogashira, Heck, Hartwig-Buchwald, and carbonylation processes into libraries of medicinally relevant heterocycles. The synthesis of libraries of indoles, benzofurans, benzothiophenes, isocoumarins and pyrones, cyclic imidates, isoxazoles, furans using this approach is reviewed. This technology is very versatile, proceeds under mild reaction conditions in high yields, and tolerates considerable functionality.
功能取代炔烃的碘环化反应为制备多种碘杂环化合物提供了一种出色的方法，这些碘杂环化合物随后可通过钯催化的铃木-宫浦反应、 Sonogashira反应、Heck反应、Hartwig-Buchwald反应以及羰基化反应，轻松地转化为具有药用价值的杂环化合物库。本文综述了使用该方法合成吲哚、苯并呋喃、苯并噻吩、异香豆素和吡喃、环状亚胺、异恶唑、呋喃等化合物库的情况。该技术用途广泛，在温和的反应条件下以高产率进行，并且能够耐受相当多的官能团。
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