4389-45-1Relevant articles and documents
Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment
Chai, Jianqi,Chen, Min,Jin, Fei,Kong, Xiangyi,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
, (2021/08/03)
Developing novel fungicide candidates are intensively promoted by the rapid emergences of resistant fungi that outbreak on agricultural production. Aiming to discovery novel antifungal leads, a series of 1,3,4-oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment were constructed for evaluating their inhibition effects against phytopathogenic fungi in vitro and in vivo. Systematically structural optimizations generated the bioactive molecule I32 that was identified as a promising inhibitor against Rhizoctonia solani with the in vivo preventative effect of 58.63% at 200 μg/mL. The observations that were captured by scanning electron microscopy and transmission electron microscopy demonstrated that the bioactive molecule I32 could induce the sprawling growth of hyphae, the local shrinkage and rupture on hyphal surfaces, the extreme swelling of vacuoles, the striking distortions on cell walls, and the reduction of mitochondria numbers. The above results provided an indispensable complement for the discovery of antifungal lead bearing a quinazolin-4(3H)-one and 1,3,4-oxadiazole fragment.
Preparation method of 2-amino-3-methyl-5-chlorobenzoic acid
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, (2021/05/12)
The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of 2-amino-3-methyl-5-chlorobenzoic acid. The preparation method provided by the invention comprises the steps of mixing m-toluic acid and nitric acid, and carrying out nitration reaction to obtain 2-nitro-3-methyl benzoic acid, wherein the mass concentration of the nitric acid is 60-75%; mixing the 2-nitro-3-methyl benzoic acid, a hydrogenation reduction reaction solvent and a hydrogenation catalyst, and carrying out hydrogenation reduction reaction in a hydrogen atmosphere to obtain 2-amino-3-methyl benzoic acid; and mixing the 2-amino-3-methyl benzoic acid, a chlorination reagent, benzoyl peroxide and a chlorination reaction solvent, and carrying out a chlorination reaction to obtain the 2-amino-3-methyl-5-chlorobenzoic acid. The preparation method provided by the invention has the advantages of cheap and easily available reaction raw materials, high product yield and high purity, and is easy for industrial production.
AN IMPROVED HYDROGENATION PROCESS USING A TRANSITION METAL COMPLEX CATALYST
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Page/Page column 27-28, (2021/07/31)
The present invention relates to the process of reduction of compound of formula (II) by using a transition metal complex (Z) as a catalyst for hydrogenation reactions to get compound of formula (I). More particularly, the present invention relates to an improved process for the preparation of a compound (I) (as described herein) or a salt thereof; comprising hydrogenation of the compound (II) (as described herein) using a transition metal complex catalyst (Z).