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Updated: Jun 12, 2025

Imine Metathesis by Silica-Supported Catalysts Using the Methodology of Surface Organometallic Chemistry
Published on: October 18, 2019
Silane-mediated, facile C-H and N-H methylation using formaldehyde
Jabir Khan1, Neha Taneja1, Naveen Yadav1
1Department of Chemistry, Indian Institute of Technology Delhi, Hauz Khas, New Delhi, 110016, India. Chinmoy.Kumar.Hazra@chemistry.iitd.ac.in.
Abstract:
The use of (para)-formaldehyde for the methylation/alkylation of C(sp2)-H and N-H bonds, utilizing a combination of silane and hexafluoroisopropanol (HFIP) as activators, is reported. Overcoming the complexity of C(sp2)-H methylation on aryl and indole substrates, the process utilizes a Friedel-Crafts alkylation, followed by silane as a hydride donor, under a mild acidic medium. The method has been employed for the synthesis of the antifungal drug butenafine and a derivative of the non-steroidal anti-inflammatory drug (NSAID) flurbiprofen.
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