- A sulfonamide - 2, 6 - dimethoxy pyrimidine preparation method (by machine translation)
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The invention relates to a sulfonamide - 2, 6 - dimethoxy pyrimidine of the preparation method, the 4 - amino - 2, 6 - dimethoxy pyrimidine and P-acetyl amino sulfonyl chloride in N, N - dimethyl formamide and the presence of triethylamine, in the 15 - 20 °C reaction under 10 - 14 hours, then post-processed to obtain 4 - P-acetyl amino sulfonamide - 2, 6 - dimethoxy pyrimidine; will be 4 - P-acetyl amino sulfonamide - 2, 6 - dimethoxy pyrimidine in methanol and the mass concentration is 15% -25% of sodium hydroxide solution in the presence of, in 85 - 90 °C reaction 5 - 7 hours, then post-processed to obtain the sulfonamide - 2, 6 - dimethoxy pyrimidine. The invention the synthetic route and the optimization of the process conditions and the like, so that the realization of the kg sulfonamide - 2, 6 - dimethoxy pyrimidine at the time of preparation, sulfonamide - 2, 6 - dimethoxy pyrimidine yield and purity of the still very high, is suitable for industrial production. (by machine translation)
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Paragraph 0023-0026; 0032-0034; 0038; 0039; 0043; 0044
(2017/12/05)
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- Evaluation of antimicrobial agents for veterinary use in the ecotoxicity test using microalgae
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The influence of antimicrobial agents approved as veterinary drugs in Japan on the growth of green algae, Selenastrum capricornutum and Chlorella vulgaris, was studied in accordance with the OECD guidelines for testing chemicals. Among the agents tested, growth inhibitory activity was very varied, i.e. erythromycin showed the strongest activity (EC50, 50% effective concentration, =0.037 mg/l), sulfa drugs had activity to some extent (EC 50s of sulfamethoxazole, sulfadiazine, and sulfadimethoxine were 1.5, 2.2, and 2.3 mg/l, respectively), but ampicillin and cefazolin did not inhibit growth (EC50s > 1000 mg/l). We also investigated synergistic effect of combining sulfa drugs with trimethoprim or pyrimethamine, which are commonly used as a combined drug. By adding trimethoprim, the growth inhibitory activity of sulfamethoxazole and sulfadiazine was significantly enhanced. Growth inhibition by sulfa drugs was reduced by the addition of folic acid, indicating that they inhibit folate synthesis in green algae.
- Eguchi, Kaoru,Nagase, Hiroyasu,Ozawa, Manao,Endoh, Yuuko S.,Goto, Kisako,Hirata, Kazumasa,Miyamoto, Kazuhisa,Yoshimura, Haruo
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p. 1733 - 1738
(2007/10/03)
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