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Syn- versus anti-carbopalladation of alkynes with organoborons: access to indoles symmetrically and unsymmetrically substituted on their 2,3-positions

Chemical Communications, ISSN: 1364-548X, Vol: 59, Issue: 45, Page: 6873-6876
2023
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Article Description

A palladium (ii)-catalyzed borono-ortho-CH activation/amination cascade for the construction of two C-N bonds and one C-C bond in a single synthetic sequence is reported. This method proceeds through a formal syn-carbopalladation of alkynes with organoboron compounds, forming alkenyl palladium species, which are trapped by simple amines to provide highly substituted indoles. Remarkably, with an electron-rich arylboronic acid, the reaction proceeds through an unexpected anti-carbopalladation terminated by ortho-CH activation of diarylalkyne/amination reaction to provide an unsymmetrically substituted 2,3-diaryl indole instead. In the follow-up chemistry, we demonstrate that urea participates in this cascade to offer a variety of free NH-indoles.

Bibliographic Details

Ghasemi, Mehran; Rahimi, Banafshe; Dehghan, Maryam; Bernoosha, Mohammad Hossein; Jafarpour, Farnaz

Royal Society of Chemistry (RSC)

Materials Science; Chemical Engineering; Chemistry

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