2454-40-2Relevant academic research and scientific papers
Synthesis and biological evaluation of quinazoline-4-thiones
Kubicova, Lenka,Sustr, Martin,Kral'ova, Katarina,Chobot, Vladimir,Vytlacilova, Jitka,Jahodar, Ludek,Vuorela, Pia,Machacek, Milos,Kaustova, Jarmila
, p. 756 - 769 (2003)
Several 2,2-dimethyl-3-phenyl-1,2-dihydroquinazoline-4(3H)-thiones and 2-methyl-3-phenylquinazoline-4(3H)-thiones were synthesized and tested for their antimycobacterial, photosynthesis-inhibiting, and antialgal activity. Antimycobacterially active compounds were found among the 6-chloro substituted compounds. 6-Chloro-3-(4-isopropylphenyl)-2-methylquinazoline-4(3H)-thione exhibited higher activity than the isoniazid standard against Mycobacterium avium and M. kansasii. Most of the compounds possessed photosynthesis-inhibiting activity. 6-Chloro-2,2-dimethyl-3-phenyl-1,2-dihydro-quinazoline-4(3H)-thione and its 3′-chloro- and 3′,4′-dichloro analogs were most effective in the inhibition of oxygen evolution rate in spinach chloroplasts. Of compounds selected for toxicological screening, 6-chloro-3-(4-isopropylphenyl)- 2-methyl-quinazoline-4(3H)-thione was the only one active in the brine shrimp bioassay.
Method for synthesizing 3-substituted aminobenzo [c] isothiazole derivative
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Paragraph 0071-0073, (2020/12/29)
The invention provides a method for synthesizing a 3-substituted aminobenzo [c] isothiazole derivative, which comprises the following steps: by using an amide N-substituted benzamide compound as an initial raw material, carrying out carbonyl oxygen sulfur replacement reaction and cyclization reaction to obtain the 3-substituted aminobenzo [c] isothiazole derivative. According to the method for synthesizing the 3-substituted aminobenzo [c] isothiazole derivative, the whole synthesis route is short in step, good in repeatability, mild in operation condition and high in safety, large-scale production and industrial popularization are facilitated, application of green and environment-friendly industrial production is facilitated, and wide application prospects are achieved.
