Liedtke Andy J, Kim Kwangho, Stec Donald F, Sulikowski Gary A, Marnett Lawrence J
A.B. Hancock Jr. Memorial Laboratory for Cancer Research, Departments of Biochemistry, Chemistry and Pharmacology, Vanderbilt Institute of Chemical Biology, Center in Molecular Toxicology and Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Tetrahedron. 2012 Dec 2;68(48):10049-10058. doi: 10.1016/j.tet.2012.08.044.
A library of approximately 40 N(1)-acylated (aza)indole alkanoic esters and acids was prepared employing a microwave-assisted approach. The optimized synthetic route allows for parallel synthesis, variation of the indole substitution pattern and high overall yield. Additionally, the procedure has been scaled up to yield multi-gram amounts of preferred indole compounds, e.g.: 2'-des-methyl indomethacin 2. The reported compounds were designed as biomedical tools for primary and secondary in vitro and in vivo studies at relevant molecular targets.
采用微波辅助方法制备了一个包含约40种N(1)-酰化（氮杂）吲哚链烷酸酯和酸的文库。优化后的合成路线允许平行合成、吲哚取代模式的变化以及较高的总收率。此外，该方法已扩大规模以生产多克量的优选吲哚化合物，例如：2'-去甲基吲哚美辛2。所报道的化合物被设计为用于在相关分子靶点进行一级和二级体外及体内研究的生物医学工具。
