Published July 2005 | Version v1
Journal article

Synthesis of (±)-kigelin

  • 1. Quaid-I-Azam University, Islamabad (Pakistan). Dept. of Chemistry

Description

A simple synthesis of racemic 8-hydroxy-6,7-dimethoxy-3-methyl-3,4-dihydroisocoumarin or kigelin, a metabolite of Aspergillus terreus and Kigelia pinnata, exhibiting several bioactivities, is described. 3,4,5-Trimethoxyhomophthalic acid was refluxed with acetic anhydride in dry pyridine to afford 2,3,4-trimethoxy-6-(2-oxopropyl)benzoic acid. Reduction of the latter followed by cyclodehydration yielded 6,7,8-trimethoxy-3-methyl-3,4-dihydroisocoumarin which on regioselective demethylation furnished the (±)-kigelin. (author)

Availability note (English)

Available from http://www.scielo.br/pdf/jbchs/v16n4/25347.pdf

Additional details

Publishing Information

Journal Title
Journal of the Brazilian Chemical Society
Journal Volume
16
Journal Issue
4
Journal Page Range
p. 739-742
ISSN
0103-5053
CODEN
JOCSET

Optional Information

Notes
17 refs., 1 fig., 2 schemes