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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Research Article

K2CO3-Promoted Highly Selective N-Hydroxymethylation of Indoles Under Metal- and Lewis Acid-Free Conditions

Author(s): Xiao-Yu Zhou* and Xia Chen

Volume 18, Issue 2, 2021

Published on: 28 July, 2020

Page: [160 - 165] Pages: 6

DOI: 10.2174/1570178617999200728214752

Price: $65

Abstract

Inorganic base promoted highly selective N-hydroxymethylation of indole and its derivatives have been developed. It provided a simple method for the preparation of N-hydroxymethyl indoles with polyformaldehyde as reagents under the metal- and Lewis acid-free reaction conditions. The reaction proceeded smoothly using K2CO3 as base in 1,4-dioxane to produce the corresponding N-hydroxymethyl indoles with 62%->99% yields.

Keywords: Indoles, hydroxymethylation, polyformaldehyde, base-promoted, functionalization, highly selective.

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