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Updated: Jun 30, 2025

Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Rhodium(II)-Catalyzed Denitrogenative Annulation for the Synthesis of Substituted Tetrahydroisoquinolines
Dun-Yuan Jin1, Chia-Wei Lin1, Srinath Santhanam1
1Department of Chemistry, National Sun Yat-sen University, Kaohsiung 804, Taiwan 70 Lienhai Road, Kaohsiung 80424, Taiwan.
Abstract:
Tetrahydroisoquinoline (THIQ) derivatives stand out as a promising class of compounds due to their diverse range of biological activities, making them particularly valuable in drug discovery. To enhance their structural diversity, an Rh-catalyzed denitrogenative annulation method has been introduced for synthesizing these derivatives. An intriguing aspect of this method is the ability of the Brønsted acid to prevent further annulation while facilitating the production of the desired THIQ derivatives, achieving impressive yields of up to 86%. This synthetic approach was subsequently leveraged to create an analogue of cyclocelabenzine, a compound showing potential as an anti-inflammatory agent.
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