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Report | Regular issue | Vol 9, No. 10, 1978, pp.1437-1439
Published online, 1st January, 1970
DOI: 10.3987/R-1978-10-1437
A Simple Synthesis of 9-Aryltheophenyllines and 9-Aryl-8-azatheophyllines

Keitaro Senga,* Yukako Kanamori, and Sadao Nishigaki

*Pharmaceutical Institute, School of Medicine, Keio University, Shinanomachi 35, Shinjuku, Tokyo 160-0016, Japan

Abstract

Treatment of 6-arylamino-1,3-dimethyluracils (I) with diazotized aniline gave 6-arylamino-l,3-dimethyl-5- phenylazouracils (11). Reductive cyclization of (11) with sodium dithionite in formic acid afforded 9-aryl- theophyllines (111). Catalytic reduction of (11) with palladium charcoal and subsequent in situ treatment with sodium nitrite and hydrochloric acid yielded 9- aryl-8-azatheophyllines (IV) .