177-04-8Relevant articles and documents
Design, synthesis and evaluation of novel trichloromethyl dichlorophenyl triazole derivatives as potential safener
Guo, Ke-Liang,Zhao, Li-Xia,Wang, Zi-Wei,Rong, Shu-Zhe,Zhou, Xiao-Lin,Gao, Shuang,Fu, Ying,Ye, Fei
, (2019/10/22)
The dominance of safener can unite with herbicides acquiring the efficient protection of crop and qualifying control of weeds in agricultural fields. In order to solve the crop toxicity problem and exploit the novel potential safener for fenoxaprop-P-ethyl herbicide, a series of trichloromethyl dichlorobenzene triazole derivatives were designed and synthesized by the principle of active subunit combination. A total of 21 novel substituted trichloromethyl dichlorobenzene triazole compounds were synthesized by substituted aminophenol and amino alcohol derivatives as the starting materials, using cyclization and acylation. All the compounds were unambiguously characterized by IR,1H-NMR,13C-NMR, and HRMS. A greenhouse bioassay indicated that most of the title compounds could protect wheat from injury caused by fenoxaprop-P-ethyl at varying degrees, in which compound 5o exhibited excellent safener activity at a concentration of 10 μmol/L and was superior to the commercialized compound fenchlorazole. A structure–activity relationship for the novel compounds was determined, which demonstrated that those compounds containing benzoxazine groups showed better activity than that of oxazole-substituted compounds. Introducing a benzoxazine fragment and electron-donating group to specific positions could improve or maintain the safener activity for wheat against attack by the herbicide fenoxaprop-P-ethyl. A molecular docking model suggested that a potential mechanism between 5o and fenoxaprop-P-ethyl is associated with the detoxication of the herbicide. Results from the present work revealed that compound 5o exhibited good crop safener activities toward wheat and could be a promising candidate structure for further research on wheat protection.
Synthesis, crystal structure and bioactivity of nphenoxyacetyl- 2-substituted-1,3-oxazolidines
Ye, Fei,Li, Na,Zhao, Li-Xia,Gao, Shuang,Fu, Ying
, p. 127 - 131 (2019/01/18)
A series of novel N-phenoxyacetyl-1,3-oxazolidine derivatives were synthesized by the cyclization and acylation with ethanolamine, ketone and phenoxyacetyl chloride as the starting materials. The structures of all the compounds were characterized by IR,
Synthesis and biological evaluafion of some new alicyclicspiro-2′- (1′, 3′ -oxazolidine) derivatives
Faidallah, Hassan M.,Sharshira,Al-Saadi, Mohammed S.M.
experimental part, p. 43 - 50 (2010/03/01)
Condensation of cyclic ketones 1 with ethanolamines gave the corresponding spiro-oxazolidines 2. The thioamides 3 were obtained in good yields through reaction of 2 with the appropriate isothiocyanate. Reaction of 2 with formaldehyde or acetaldehyde in the presence of the appropriate amine afforded the corresponding aminomethyl spiro-compounds 4 and 5 respectively, in excellent yields. The structures of the isolated compounds were fully determined by spectral methods. Antimicrobial activities of some oxazolidines were also discussed.