thionamides. I. Synthesis. Demethylation of their N, N-Dimethyl Derivatives by Sulfur.

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概要

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• Methylpyrazine (I) and 2-picoline (VI) were converted to N, N-dimethylpyrazinecar-bothionamide and N, N-dimethylpicolinethionamide (II and VII) respectively on fusion with sulfur in dimethylformamide. Iodine was found effective as a catalyst for the reaction. Besides the ordinal products (II and VII), the corresponding demethylated products were also isolated, thus indicating that the demethylation reaction, presumably due to the action of sulfur, was involved. The demethylation reaction was confirmed by the formation of N-methylpyrazinecarbothionamide and N-methylpicolinethionamide (III and VIII) from II and VII respectively on fusion with sulfur. II was 4 times more effective than pyrazinecarboamide against M. tuberculosis and its toxity was LD_<50> 1180±15 mg./kg.

• 公益社団法人日本薬学会の論文
• 1963-04-25

著者

• 義平 邦利

  九州大学薬学部

• 義平 邦利

  Institute of Medical Sciences

• 義平 邦利

  National Institute Of Hygienic Science

• 田口 胤三

  Faculty of Pharmaceutical Sciences, Kyushu University

• 田口 胤三

  Institute of Pharmaceutical Sciences, Faculty of Medicine, Kyushu University

• 田口 胤三

  Faculty Of Pharmaceutical Sciences Kyushu University

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