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Communication | Regular issue | Vol 16, No. 1, 1981, pp.21-24
Published online, 1st January, 1970
DOI: 10.3987/R-1981-01-0021
Introducing Amino Group on 1(2H)-Phthalazinone Derivatives

Masayuki Ishikawa,* Yukuo Eguchi, and Akiko Sugimoto

*Tokyo Medical and Dental University, 2-3-10, Surugadai, Kanda, Chiyoda-ku 101-0062, Japan


Nitration of 4-ethoxycarbonyl-1(2H)-phthalazinone (4) with KNO3 and conc sulfuric acid at room temperature afforded the corresponding 5-nitro derivative (5) in about 50% yield. The latter compound was converted to 5-acetylamino-4-hydroxymethyl-1(2H)-phthalazinone (9). The preparation of 4-amino-7-ethoxycarbonyl-6,8-dimethyl-1(2H)-phthalazinone (13) through the Curtius reaction of the hydrazide (10) was also described.