98092-65-0Relevant articles and documents
Extending the versatility of the Hemetsberger-Knittel indole synthesis through microwave and flow chemistry
Ranasinghe, Nadeesha,Jones, Graham B.
, p. 1740 - 1742 (2013/04/10)
Microwave, flow and combination methodologies have been applied to the synthesis of a number of substituted indoles. Based on the Hemetsberger-Knittel (HK) process, modifications allow formation of products rapidly and in high yield. Adapting the methodology allows formation of 2-unsubstituted indoles and derivatives, and a route to analogs of the antitumor agent PLX-4032 is demonstrated. The utility of the HK substrates is further demonstrated through bioconjugation and subsequent ring closure and via Huisgen type [3+2] cycloaddition chemistry, allowing formation of peptide adducts which can be subsequently labeled with fluorine tags.