- Preparation method of carbendazim
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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.
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Paragraph 0015
(2021/08/25)
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- Synthesis and antimicrobial activity of benzazolyl azolyl urea derivatives
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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.
- Narendra babu, Kayathi,Nagarjuna, Ummadi,Reddy, Guda Dinneswara,Padmaja, Adivireddy,Padmavathi, Venkatapuram
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- Carbendazim preparation technology
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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.
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Paragraph 0007; 0015
(2017/01/17)
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- Design and synthesis of novel benzoheterocyclic derivatives as human acrosin inhibitors by scaffold hopping
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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.
- Chen, Qianqian,Tian, Wei,Han, Guangqian,Qi, Jingjing,Zheng, Canhui,Zhou, Youjun,Ding, Lili,Zhao, Juntao,Zhu, Ju,Lv, Jiaguo,Sheng, Chunquan
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p. 176 - 182
(2013/03/13)
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- Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H- benzo[d]imidazol-2-yl carbamate derivatives
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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.
- Liu, Xuefei,Chen, Qianqian,Zhu, Ju,Fan, Yongzheng,Ding, Lili,Zhao, Juntao,Han, Guangqian,Tian, Wei,Qi, Jingjing,Zhou, Youjun,Lv, Jiaguo
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scheme or table
p. 3554 - 3559
(2012/06/18)
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- Acyl derivatives of 2-aminobenzimidazole and their fungicide activity
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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.
- Pilyugin,Sapozhnikov,Sapozhnikova
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p. 738 - 743
(2007/10/03)
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- Synthesis and antiparasitic activity of 1H-benzimidazole derivatives.
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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.
- Valdez, Juan,Cedillo, Roberto,Hernandez-Campos, Alicia,Yepez, Lilian,Hernandez-Luis, Francisco,Navarrete-Vazquez, Gabriel,Tapia, Amparo,Cortes, Rafael,Hernandez, Manuel,Castillo, Rafael
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p. 2221 - 2224
(2007/10/03)
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- Synergistic biocide composition
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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.
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- Agricultural and horticultural fungicidal composition
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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.
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- N-alkyl-2,6-dimethylmorpholinocarboxamide salts, compositions and their use as fungicides
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Novel N-alkyl-2,6-dimethylmorpholinocarboxamide salts of the general formula I, STR1 processes for their preparation, and their use as fungicides for controlling pathogenic fungi. The agents according to the invention additionally possess plant growth-regulating properties. The meanings of R1, R2, R3, R4 and X- are given in the description. (Formula I)
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- Biocidal tributyltin compounds
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Tri-n-butylstannyloxy tricyclodecanes, their preparation, and biocidal agents containing the same as active ingredients.
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- Organosilyl compounds and their use as fungicides
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Organosilyl compounds of the general formula I STR1 where R1, R2 and R3 are alkyl, substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted aryl, R4 and R5 are alkyl or hydrogen and Y is CH2, oxygen, nitrogen or alkyl-substituted nitrogen, their salts and fungicides containing these compounds.
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- Process for reducing the proportions of by products in the preparation of carbendazim
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The invention relates to a process for the preparation of highly pure carbendazim STR1 which starts from o-phenylenediamine and methyl cyanocarbamate, and, in addition, a reducing agent is added.
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- 4-Nitro-2-trichloromethylphenylsulfenamides
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New 4-nitro-2-trichloromethylphenylsulfenamides having a fungicidal and bactericidal action, processes for their manufacture, fungicides containing these compounds as active ingredients, and a process for combating fungi with these compounds.
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- Thiolphosphoric acid-S-4-nitro-2-trichloromethylphenyl esters as fungicides
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New thiolphosphoric acid-S-4-nitro-2-trichloromethylphenyl esters of the formula STR1 where X denotes oxygen or sulfur, and R1 and R2 are identical or different and each denotes a substituted or unsubstituted aliphatic radical of 1 to 18 carbon atoms or a substituted or unsubstituted alicyclic radical of 5 to 18 carbon atoms, processes for their manufacture, fungicides containing these compounds as active ingredients, their manufacture, and processes for combating fungi with these novel compounds.
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- Asymmetric Chloral Aminals, Derivatives of Benzimidazole and Benzothiazole.
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In the report research program, a series of chloral aminals have been synthesized. They contain, as substituents at both the nitrogen atoms: aryloxyacetyl residue, and N-(2-benzothiazole), N-(2-benzimidazole) or N-(2-carbomethoxyamino) benzimidazole rests. Compounds of this type of expected biological activity as pesticides have been prepared by transformation of N-aryloxyacetylchloral semiaminals into N-(1,2,2,2-tetrachloroethyl) aryloxyacetamides and by reaction of the latter with 2-aminobenzimidazole, 2-aminobenzothiazole or carbendazin.
- Barczynski,Jedrzejkowski,Eckstein
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p. 303 - 304
(2007/10/04)
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- 3-(Haloalkoxyalkyl)-carbamyl benzimidazolyl carbamates and their use as pesticides
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Compounds of the formula: STR1 in which R1 represents a hydrogen or halogen atom, an alkyl group containing from 1 to 4 carbon atoms, an alkoxy group containing 1 to 4 carbon atoms or a nitro group, R2 represents an alkyl group containing from 1 to 4 carbon atoms, R3 represents a hydrogen atom or an alkyl or haloalkyl group containing from 1 to 4 carbon atoms, R4 represents an alkyl, haloalkyl, arylalkyl or arylhaloalkyl group containing from 1 to 12 carbon atoms, At least one of the groups R3 and R4 being a halogenated group. These compounds are systemic fungicides, antisporulants and sterilizers of acaridae eggs.
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- N-(fluorodichloromethylthio)-benzanilides
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New and valuable N-(fluorodichloromethylthio)-benzanilides, a process for their manufacture, fungicides containing these compounds as active ingredients, and a method of combatting fungi with these compounds.
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- 2-Benzimidazolecarbamic acid esters by the cyanamide process
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A process for making 2-benzimidazolecarbamic acid, alkyl esters by reacting cyanamide or a cyanamide salt with an alkyl chloroformate in a weakly acidic to basic medium at a temperature between 0° and 105° C. to form an alkyl cyanocarbamate salt; then reacting the alkyl cyanocarbamate salt with an o-phenylenediamine in an acidic medium at a temperature between 40° and 130° C. to form the desired product and recovering it from the reaction mixture. The 2-benzimidazolecarbamic acid, alkyl esters are useful as fungicides and also useful as intermediates in the preparation of dialkyl esters of 2-carboxyaminobenzimidazole-1-carboxylic acids.
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