title: Automated Multistep Continuous Flow Synthesis of 2-(1H-Indol-3-yl)thiazole Derivatives.
abstract: The multistep continuous flow assembly of 2-(1H-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-(1H-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).
authors.affiliation: 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.
authors.forename: Nicholas
authors.initials: N
authors.lastname: Pagano
authors.affiliation: Southern Research Institute, Drug Development Division, 431 Aviation Way, Frederick, MD 21701.
authors.forename: Marintha L
authors.initials: ML
authors.lastname: Heil
authors.affiliation: 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.
authors.forename: Nicholas D P
authors.initials: ND
authors.lastname: Cosford
keywords: condensation; heterocycles; indoles; microfluidic synthesis; microreactors; tandem reaction