Bioorganic & medicinal chemistry letters

Extending the versatility of the Hemetsberger–Knittel indole synthesis through microwave and flow chemistry

N Ranasinghe, GB Jones

Index: Ranasinghe, Nadeesha; Jones, Graham B. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1740 - 1742

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Citation Number: 4

Abstract

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 ...