25877-54-7

Upstream product

• 3290-99-1 4-methoxybenzoic acid hydrazide 
• 75-36-5 acetyl chloride 
• 54019-08-8 4-methoxy-benzoic acid N'-acetyl-hydrazide 
• 78-39-7 Triethyl orthoacetate 
• 14849-47-9 (E)-N'-(4-M'methoxybenzylidene)acetohydrazide 
• 18871-66-4 N,N-dimethylacetamide dimethyl acetal 
• 6926-51-8 5-(4-methoxyphenyl)-1H-tetrazole 
• 108-24-7 acetic anhydride 
• 59670-27-8 4-methoxybenzaldehyde N-acetylhydrazone 
• 127-19-5 N,N-dimethyl acetamide 
• 1445-45-0 Trimethyl orthoacetate 
• 121-98-2 methyl 4-methoxybenzoate 

Downstream Products

• 94223-54-8 4-[5-(4-Methoxy-phenyl)-[1,3,4]oxadiazol-2-yl]-butan-2-one 
• 25877-46-7 4-(5-methyl-1,3,4-oxadiazol-2-yl)phenol 
• 94223-61-7 4-Methoxy-benzoic acid N'-(5-methyl-4,5-dihydro-3H-pyrrol-2-yl)-hydrazide 
• 94223-65-1 3-(4-Methoxy-phenyl)-5-methyl-6,7-dihydro-5H-pyrrolo[2,1-c][1,2,4]triazole 

Relevant academic research and scientific papers

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.

Synthesis and spectral luminescence properties of 2-aryl-5-methyl-1,3,4-oxadiazoles and zinc(ii) 2-(2-hydroxyphenyl)-5-methyl-1,3,4-oxadiazole complex

2-Aryl-5-methyl-1,3,4-oxadiazoles were synthesized by reflux of equimolar amounts of acyl hydrazides with triethyl orthoacetate in o-xylene. The obtained oxadiazoles, except for 2-(2-hydroxyphenyl)-5-methyl-1,3,4-oxadiazole, luminesce with a high quantum

TiCl4 mediated facile synthesis of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles

An efficient method for the synthesis of 2,5-disubstituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles has been developed. Various hydrazides or thionyl hydrazides readily react with DMA derivatives in the presence of TiCl4 as a catalyst to afford the desired products. This protocol provides a simple and economical procedure that affords the target products with good yields and wide substrate scope.

Metal-Free Synthesis of 1,3,4-Oxadiazoles from N′-(Arylmethyl)hydrazides or 1-(Arylmethyl)-2-(arylmethylene)hydrazines

An efficient and versatile metal-free synthesis of 1,3,4-oxadiazoles from N′-(arylmethyl)hydrazides or 1-(arylmethyl)-2-(arylmethylene)hydrazines through oxidative dehydrogenation is reported. A range of 2,5-disubstituted 1,3,4-oxadiazoles were prepared by treating N′-(arylmethyl)hydrazides with (diacetoxyiodo)benzene in acetonitrile or by treating 1-(arylmethyl)-2-(arylmethylene)hydrazines with [bis(trifluoroacetoxy)iodo]benzene in methyl tert-butyl ether. Aldehyde N-acylhydrazones and aldazines were initially generated in situ as intermediates.

Microwave promoted one-pot synthesis of 2-aryl substituted 1,3,4-oxadiazoles and 1,2,4-oxadiazole derivatives using Al3+-K10 clay as a heterogeneous catalyst

An efficient, inexpensive method is developed for the one-pot synthesis of 2-aryl substituted 1,3,4-oxadiazoles and 1,2,4-oxadiazoles starting from acid hydrazides and trimethyl orthoformate under solvent-free, microwave conditions using a reusable Alsup

Iodine-catalysed oxidative cyclisation of acylhydrazones to 2,5-substituted 1,3,4-oxadiazoles

An environmentally benign synthesis of 2,5-disubstituted 1,3,4-oxadiazoles has been developed starting from N-aroylhydrazones and N-acetylhydrazones at room or ambient temperature using a catalytic quantity of iodine in the presence of an aqueous hydrogen peroxide oxidant.

Efficient synthesis of 1,3,4-oxadiazoles promoted by NH4Cl

An efficient and inexpensive approach to the synthesis of 2-substituted and 2,5-disubstituted 1,3,4-oxadiazoles from arylhydrazides and orthoesters is reported using catalytic NH4Cl. The conditions are mild, and thus, compatible with a variety of functional groups. The optimized reaction is performed using 30 mol % of NH4Cl in 100% EtOH and is generally complete within 1 h for non-aromatic orthoesters and 2-10 h for aromatic orthoesters. The reaction permits both electron-releasing and electron-withdrawing groups on the arylhydrazide substrate. Most products are formed in high yields and require only minimal purification. Compared with earlier reports, the current reactions proceed in shorter time and require less of the orthoester.

One-pot synthesis of 2,5-disubstituted-1,3,4-oxadiazoles based on the reaction of N,N-dimethyl amides with acid hydrazides

Convenient and efficient one pot method for the synthesis of 2,5-disubstituted-1,3,4-oxadiazoles based on the reaction of N,N-dimethyl amides with acid hydrazides has been developed. The methodology is applied to a wide range of difference aryl hydrazide and difference N,N-dimethyl amides to 2,5-disubstituted-1,3,4-oxadiazoles yield the in good to excellent yields. It will be possible wide useful application in synthesis. Synopsis Convenient and efficient one pot method for the synthesis of 2,5-disubstituted-1,3,4- oxadiazoles based on the reaction of N,N-dimethyl amides with acid hydrazides has been developed. The methodology is applied to a wide range of difference aryl hydrazide and difference N,N-dimethyl amides to 2,5-disubstituted- 1,3,4-oxadiazoles yield the in good to excellent yields. It will be possible wide useful application in synthesis. Copyright

Synthesis, characterization, and antimicrobial evaluation of oxadiazole congeners

A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, 1H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram-ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram-ve bacteria, or fungal cells used in the present study.

Tetrazoles: LIII. Microwave-activated acylation of 5-substituted tetrazoles

The acylation of 5-aryl(hetaryl)tetrazoles with acetic and benzoic anhydrides under microwave irradiation gave the corresponding 2-substituted 5-methyl-and 5-phenyl-1,3,4-oxadiazoles in high yields. The use of microwave activation reduces the reaction temperature by 30-40°C and shortens the reaction time by a factor of 5 to 7.