326829-08-7Relevant articles and documents
Discovery of novel 3-{[(5,5-dimethyl-4,5-dihydroisoxazol-3-yl)sulfonyl]methyl}benzo[d]isoxazole analogs as promising very long chain fatty acids inhibitors
Lin, Jian,Li, Yitao,Hu, Xiaoyun,Chi, Weilin,Zeng, Shuiming,Xu, Junxing
, p. 226 - 240 (2020/10/19)
Very long chain fatty acids (VLCFAs) are one of the most principal and promising targets for herbicides discovery. In order to explore and find novel VLCFAs inhibitors with higher herbicidal activity and improved crop safety, a variety of new 3-{[(5,5-dimethyl-4,5-dihydroisoxazol-3-yl)sulfonyl]methyl}benzo[d]isoxazole derivatives were reasonably designed and synthesized. The results of greenhouse experiments indicated that several compounds exhibited good herbicidal activity against Digitaria sanguinalis, Echinochloa crus-galli, and Setaria faberii at rates of 150 g ai/ha. Compounds g4 and h1 displayed promising herbicidal activity against D sanguinalis and E crus-galli at rates of 75 g ai/ha, which is better than commercial pyroxasulfone and S-metolachlor. Moreover, compound h1 displayed higher activity against E crus-galli, D sanguinalis, and S faberii than pyroxasulfone and S-metolachlor even at a rate of 37.5 and 18.75 g ai/ha. Furthermore, both of the compounds g4 and h1 were much safer to these tested crops, especially to rice, wheat and rape, at the rate of 150 g ai/ha than pyroxasulfone. Therefore, h1 may act as a new lead structure for novel herbicides discovery.
Method for preparing pyroxasulfone intermediate 5, 5-dimethyl-4, 5-dihydroisoxazole-3-thioformamidine hydrochloride
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Paragraph 0056-0057; 0063-0065; 0067-0068; 0070-0072, (2021/04/14)
The invention relates to the field of pesticide herbicide synthesis, in particular to a method for preparing a sulfonylpyraflufen-ethyl intermediate 5, 5-dimethyl-4, 5-dihydroisoxazole-3-thioformamidine hydrochloride, which comprises the following steps: reacting a compound IV with strong acid to form salt to obtain a compound III; directly carrying out chlorination reaction on the compound III and chlorine without purification to obtain a chlorination product compound II; and reacting the compound II with thiourea in an organic solvent in the presence of inorganic acid to obtain a compound I. According to the method, the compound IV is used as a raw material, the raw material cost is low, salifying and chlorination are performed to obtain the product compound II, byproducts are few, reaction operation is easy and convenient, and pollution is small; AND finally, the compound I is prepared by directly reacting with thiourea in the presence of inorganic acid, the yield of a finished product is up to 90% or above, the purity can reach 99%, a used solvent can be completely recycled, and the method is very suitable for industrial production.
PROCESS FOR PREPARATION OF PYROXASULFONE
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Page/Page column 21-22, (2020/12/11)
The present invention discloses a process for the preparation of Pyroxasulfone of Formula (I) or salt thereof. Particularly, the present invention discloses an improved process for the preparation of hydroxycarbonimidic dibromide compound of Formula (III) or salt thereof, wherein bromine anion is recycled by using a suitable oxidizing agent. Moreover, the present invention relates to a continuous flow process for preparing of compound of Formula (I) or salt thereof.
