发明名称 AMINO AND AMIDO DERIVATIVES OF CHLORO NITRO AMINO AND ALKYLAMINO PYRAZINES USEFUL AS ADJUNCTS TO RADIATION THERAPY
摘要 2-Substituted amino derivatives of 6-amino-3-chloro-5-nitropyrazin-2-yl are prepared by converting 3-amino-5,6-dichloropyrazinecarboxylic acid to 5,6-dichloro-3-nitropyrazinamine and treating said compound with an amine to produce the corresponding 2-substituted amino compound. 2,6-Di(alkylamino) derivatives of chloronitropyrazines are prepared from dichloronitropyrazinamine by diazotization of the amine followed by halogen exchange to produce an intermediate dichloro-halo nitropyrazine followed by reaction with one or two moles of an alkyl amine to effect replacement of one or two of the pyrazine halogens. N-acyl derivatives of 6-(alkylamino)-5-chloro-3-nitropyrazinamines are prepared by treatment of 5,6-dichloro-3-nitropyrazinamine with an acylating agent to produce the corresponding acylated pyrazinamine followed by treatment of said acylate dpyrazinamine with a lower alkylamine to replace one of the chloro substituents and produce a 2-acylamino-6-(alkylamino)-5-chloro-3-nitro pyrazinamine.
申请公布号 DE3274980(D1) 申请公布日期 1987.02.12
申请号 DE19823274980 申请日期 1982.06.09
申请人 MERCK & CO. INC. 发明人 HARTMAN, GEORGE D.
分类号 C07D241/16;C07D241/20;(IPC1-7):C07D241/20;A61K31/495 主分类号 C07D241/16
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