Synthesis of Polycyclic Indolines

Palladium/Norbornene Chemistry in the Synthesis of Polycyclic Indolines with Simple Nitrogen Sources: M. Ghasemi, F. Jafarpour, A. Habibi
Synthesis 2020, 52, DOI: 10.1055/s-0039-1707988


The indoline scaffold is commonly encountered in natural compounds – such as alkaloids – and drug candidates. A number of synthetic routes are available for assembling the indoline structural framework – such as the Buchwald–Hartwig amination – however, efforts towards the development of atom-economical and efficient target-specific methods for the synthesis of indolines continue to attract the interest of organic chemists. Recently, the group of Professor Farnaz Jafarpour from the University of Tehran (Iran) reported a new approach for the preparation of polycyclic indolines.

Professor Jafarpour said: “We have developed the construction of polycyclic N-alkylindolines via amination of an aryl-norbornene-palladacycle as the key intermediate in Pd/NBE chemistry, employing readily available nitrogen sources such as aliphatic amines and ureas without using any additional ligands.”

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