Gallou, Fabrice (2020) Development of a robust protocol for the synthesis of 6-hydroxybenzofuran-3-carboxylic acid. Organic process research & development, 24 (5). pp. 861-866. ISSN 1520-586X; 1083-6160

Abstract

Benzofuran scaffolds are fundamental moieties found in a variety of biologically active natural products and synthetic drugs. In the course of one of our development programs, we needed to develop a practical and cost-effective manufacturing approach to such a benzofuran scaffold. Here, a 4-step 1-pot process is reported, allowing the access to a 6-hydroxybenzofuran-3-carboxylic acid structure as highly robust. A 1H NMR monitoring study allowed a better understanding of the overall sequence of event and the nature of the detected intermediates. After 6 steps, including the optimized tandem process, the desired hydroxylated benzofuran was obtained with 40% yield and a purity above 99%.

Item Type:	Article
Date Deposited:	30 Jun 2020 00:45
Last Modified:	30 Jun 2020 00:45
URI:	https://oak.novartis.com/id/eprint/41568