T. Aono, S. Kishimoto, Y. Araki
Dec 25, 1977
Citations
0
Influential Citations
6
Citations
Journal
Chemical & pharmaceutical bulletin
Abstract
The relative reactivity in each position of 1-indancarboxylic acid (IV) toward electro-hilic substitution reaction such as chlorination, bromination, acylation, sulfonation and nitration was examined and it was found that the 6-position is the most reactive. By these reactions, pharmacologically interesting meta-substituted phenylacetic acid derivatives were readily obtained. Electrophilic chlorination of IV followed by cycloalkylation provided an improved alternative synthetic method of antiinflammatory 6-chloro-5-cyclohexyl-1-indancarboxylic acid (TAI-284, I) and its analogs.