A Catalytic One-Pot Synthesis of Indolyl Cyclobutanones

A Catalytic One-Pot Synthesis of Indolyl Cyclobutanones: S. Porcu, C. A. Rodriguez, A. Frongia, F. Secci

Synthesis 2021, 53, DOI: 10.1055/s-0040-1706087


Cyclobutyl rings are privileged structures in a number of key areas, such as drug discovery and agrochemistry, besides being present in many bioactive natural compounds. However, the incorporation of strained cyclobutyl units into organic scaffolds can be challenging and the development of novel effective synthetic methods to achieve this goal continues to attract the interest of organic chemists.

Recently, the group of Dr. Francesco Secci from the Università degli Studi di Cagliari (Italy) described a general, one-pot and user-friendly strategy for the incorporation of cyclobutanone fragments onto indolyl rings.


Dr. Secci said: “New indole scaffolds were constructed by a tandem Brønsted acid catalyzed 2-hydroxycyclobutanone-activation strategy in good yields, opening new synthetic routes for medicinal chemistry purposes.”

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