110342-67-1Relevant articles and documents
Preparation method of carbendazim
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Paragraph 0015, (2021/08/25)
The invention discloses a preparation method of carbendazim. According to the method, carbendazim is prepared through acylation reaction which is mild in reaction condition and extremely high in reaction efficiency. The optimal preparation method of carbendazim is screened through a large number of experiments, the whole process is reasonable in design, and the process is easy to operate and efficient. Meanwhile, the reaction yield can be greatly increased (up to 92% or above), side reactions can be reduced, the reaction efficiency can be improved, the energy consumption required by the reaction can be reduced, the production cost can be greatly reduced, and the method has a very good application prospect.
Synthesis and antimicrobial activity of benzazolyl azolyl urea derivatives
Narendra babu, Kayathi,Nagarjuna, Ummadi,Reddy, Guda Dinneswara,Padmaja, Adivireddy,Padmavathi, Venkatapuram
, (2019/08/20)
A new class of benzazolyl azolyl urea derivatives were prepared by the reaction of methyl benzazoyl carbamates with azolyl amines in the presence of mild base potassium tert-butoxide. The presence of electron withdrawing substituents on the aromatic ring enhanced the activity. Nitro substituted benzothiazolyl thiazolyl urea, benzothiazolyl imidazolyl urea and benzimidazolyl thiazolyl urea exhibited potential antibacterial activity against Bacillus subtilis. The compound benzothiazolyl imidazolyl urea and nitro substituted benzimidazolyl imidazolyl urea showed potential antifungal activity against Aspergillus niger.
Carbendazim preparation technology
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Paragraph 0007; 0015, (2017/01/17)
The invention discloses a carbendazim preparation method. Being improved based on a traditional synthesis technology, the carbendazim preparation method is characterized in that firstly, a methylbenzene and water biphasic solvent reaction system is adopted, so that carbendazim appearance is improved, carbendazim is bright white, purity can be above 99.8% and carbendazim grade is increased; secondly, a method that concentrated hydrochloric acid and a methyl cyanocarbamate cyclizing agent are added dropwise simultaneously is adopted, and carbendazim yield can be above 97.5%. Compared with an existing traditional synthesis technology, the carbendazim preparation method has the greatest advantages that carbendazim yield is high, and the carbendazim is excellent in color and luster and high in purity, thereby being a method capable of preparing the high-quality carbendazim.
Design and synthesis of novel benzoheterocyclic derivatives as human acrosin inhibitors by scaffold hopping
Chen, Qianqian,Tian, Wei,Han, Guangqian,Qi, Jingjing,Zheng, Canhui,Zhou, Youjun,Ding, Lili,Zhao, Juntao,Zhu, Ju,Lv, Jiaguo,Sheng, Chunquan
, p. 176 - 182 (2013/03/13)
Human acrosin is an attracting target for the development of novel male contraceptives. Scaffold hopping was used to optimize the isoxazolecarbaldehyde human acrosin inhibitors and extend their structure-activity relationships. Four kinds of scaffolds, namely benzimidazole, benzothiazole, 3H-indazole, and 5-phenyl-1H-pyrazole, were designed and synthesized. Most of the synthesized compounds showed potent human acrosin inhibitory activity and their binding modes were investigated by molecular docking. The scaffold of the compounds was found to be important for the inhibitory activity. Several compounds were more active than the positive control TLCK, suggesting that they can serve as good starting points for the discovery of novel male contraceptive agents.
Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H- benzo[d]imidazol-2-yl carbamate derivatives
Liu, Xuefei,Chen, Qianqian,Zhu, Ju,Fan, Yongzheng,Ding, Lili,Zhao, Juntao,Han, Guangqian,Tian, Wei,Qi, Jingjing,Zhou, Youjun,Lv, Jiaguo
scheme or table, p. 3554 - 3559 (2012/06/18)
A series of novel methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamates were designed, synthesized, and their acrosin inhibitory activities evaluated in vitro. The results of acrosin inhibitory activity showed that all title compounds were more potent than the control TLCK. Compound 4w displayed the most potent acrosin inhibitory activity among all the compounds, with an IC 50 of 6.3 × 10-5 M. The studies provide a new structural class for the development of novel acrosin inhibitory agents.
Acyl derivatives of 2-aminobenzimidazole and their fungicide activity
Pilyugin,Sapozhnikov,Sapozhnikova
, p. 738 - 743 (2007/10/03)
Procedures have been developed for the preparation of methyl 2-benzimidazolylcarbamate, 2-acetylaminobenzimidazole, 2- benzoylaminobenzimidazole, 2-(3,5-dibromo-2-hydroxybenzoylamino)benzimidazole, 1-(3,6-dichloro-2-methoxybenzoyl)-2-aminobenzimidazole, 2-(3,5-dichloro-2- hydroxybenzoylamino)benzimidazole, 2-(3,5-dichloro-2-methoxybenzoylamino) benzimidazole, and 1-(3,5,6-trichloro-2-methoxybenzoyl)-2-aminobenzimidazole. The synthesized compounds have been tested for fungicide activity.
Synthesis and antiparasitic activity of 1H-benzimidazole derivatives.
Valdez, Juan,Cedillo, Roberto,Hernandez-Campos, Alicia,Yepez, Lilian,Hernandez-Luis, Francisco,Navarrete-Vazquez, Gabriel,Tapia, Amparo,Cortes, Rafael,Hernandez, Manuel,Castillo, Rafael
, p. 2221 - 2224 (2007/10/03)
Compounds 1-18 have been synthesized and tested in vitro against the protozoa Giardia lamblia, Entamoeba histolytica and the helminth Trichinella spiralis. Inhibition of rat brain tubulin polymerization was also measured and compared for each compound. Results indicate that most of the compounds tested were more active as antiprotozoal agents than Metronidazole and Albendazole. None of the compounds was as active as Albendazole against T. spiralis. Although only compounds 3, 9 and 15 (2-methoxycarbonylamino derivatives) inhibited tubulin polymerization, these were not the most potent antiparasitic compounds.
Synergistic biocide composition
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, (2008/06/13)
A biocide composition is provided as an addition to substances that can be infected by harmful microorganisms, in which the biocide composition has at least two active biocidal substances, one of which is 2-methylisothiazolin-3-one. The composition is characterized in that it contains 1,2-benzisothiazolin-3-one, compositions containing 5-chloro-2-methylisothiazolin-3-one being excluded. In comparison with its individual components, the composition of the invention has a synergistic biocidal activity.
Agricultural and horticultural fungicidal composition
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, (2008/06/13)
An agricultural and horticultural fungicidal composition comprising a benzothiazole derivative represented by formula (I): wherein R1 represents a lower alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an alkoxyalkyl group, a benzyl group, an alkyl group containing a carbonyl group or an alkoxyalkyl group containing a carbonyl group; and R2 represents a lower alkyl group, an alkoxy group or an alkyl group having from 1 to 3 carbon atoms and containing from 1 to 6 fluorine atoms, and a compound having a fungicidal activity is disclosed. The composition exhibits a markedly improved effect as compared to the effects of the individual use of the ingredient and is useful as the agricultural and horticultural fungicidal composition as it exhibits preventive and curing effects on plant diseases.