Pagano Nicholas, Heil Marintha L, Cosford Nicholas D P
Apoptosis and Cell Death Research Program & Conrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute, 10901 N. Torrey Pines Rd., La Jolla, CA 92037.
Southern Research Institute, Drug Development Division, 431 Aviation Way, Frederick, MD 21701.
Synthesis (Stuttg). 2012;44(16):2537-2546. doi: 10.1055/s-0031-1290953.
The multistep continuous flow assembly of 2-(-indol-3-yl)thiazoles using a Syrris AFRICA synthesis station is reported. Sequential Hantzsch thiazole synthesis, deketalization and Fischer indole synthesis provides rapid and efficient access to highly functionalized, pharmacologically significant 2-(-indol-3-yl)thiazoles. These complex, drug-like small molecules are generated in reaction times of less than 15 min and in high yields (38%-82% over three chemical steps without isolation of intermediates).
报道了使用Syrris AFRICA合成工作站对2-（-吲哚-3-基）噻唑进行多步连续流动组装。依次进行汉茨希噻唑合成、脱缩酮反应和费歇尔吲哚合成，能够快速高效地获得高度官能化、具有药理学意义的2-（-吲哚-3-基）噻唑。这些复杂的、类药物小分子在不到15分钟的反应时间内生成，产率很高（在三个化学步骤中，无需分离中间体，产率为38%-82%）。
