Work

Automated Multistep Continuous Flow Synthesis of 2-(1H-Indol-3-yl)thiazole Derivatives

Year: 2012

Type: article

Abstract: The multistep continuous flow assembly of 2-(1 H -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-(1 H -indol-3-yl)thiazoles. These complex drug-like small molecules are generated in reaction times of less than 15 minutes and in high yields (38–82% over three chemical steps without isolation of intermediates).

Source: Synthesis

DOI: 10.1055/s-0031-1290953

Authors: Nicholas Cosford, Nicholas Pagano, Marintha Heil

Institutions: Sanford Burnham Prebys Medical Discovery Institute, Southern Research Institute

Language: English

Topic: Innovative Microfluidic and Catalytic Techniques Innovation

Subfield: Biomedical Engineering

Field: Engineering

Domain: Physical Sciences

Open Access status: green

Funders: National Human Genome Research Institute, National Cancer Institute, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases

Awards: Countermeasures for Bioterroism Targeting Cellular Host Factors, Drug Discovery for Fatty Acid Synthase in Oncology, Stereochemically and Structurally Diverse Pilot Scale Libraries for the MLSMR, Highly Diverse and Structurally Varied Heterocyclic Libraries for the MLSMR, Sanford-Burnham Center for Chemical Genomics