1874-35-7

Upstream product

• 6797-81-5 4-dimethylamino-benzoic acid N'-benzoyl-hydrazide 
• 111997-55-8 1-[(4-Dimethylamino-phenyl)-methylsulfanyl-methylene]-piperidinium; iodide 
• 613-94-5 benzoic acid hydrazide 
• 31646-31-8 4-[(4-dimethylamino-phenyl)-methylsulfanyl-methylene]-morpholinium; iodide 
• 18039-42-4 5-Phenyl-1H-tetrazole 
• 7474-31-9 p-N,N-dimethylaminobenzoic anhydride 
• 14850-85-2 (E)-N′-(4-(dimethylamino)benzylidene)benzohydrazide 
• 58634-27-8 4-(dimethylamino)phenyl (piperidin-1-yl)methanethione 
• 5925-53-1 4-<4-(Dimethylamino)thiobenzoyl>morpholine 
• 1202-25-1 methyl 4-(N,N-dimethylamino)benzoate 
• 19353-92-5 4-(dimethylamino)benzohydrazide 
• 591-50-4 iodobenzene 
• 119072-55-8 tert-butylisonitrile 
• 4755-50-4 4-(dimethylamino)benzoyl chloride 

Relevant academic research and scientific papers

Palladium-catalyzed one-pot synthesis of diazoles via tert-butyl isocyanide insertion

An efficient one-pot palladium-catalyzed reaction for the synthesis of diazoles from readily available hydrazides and aryl halide via isocyanide insertion/cyclization sequence has been developed. This methodology efficiently constructs diazoles in good to excellent yields with the advantages of wide functional group tolerance and operational simplicity.

Oxadiazoles in medicinal chemistry

Oxadiazoles are five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom, and they exist in different regioisomeric forms. Oxadiazoles are frequently occurring motifs in druglike molecules, and they are often used with the intention of being bioisosteric replacements for ester and amide functionalities. The current study presents a systematic comparison of 1,2,4- and 1,3,4-oxadiazole matched pairs in the AstraZeneca compound collection. In virtually all cases, the 1,3,4-oxadiazole isomer shows an order of magnitude lower lipophilicity (log D), as compared to its isomeric partner. Significant differences are also observed with respect to metabolic stability, hERG inhibition, and aqueous solubil ity, favoring the 1,3,4-oxadiazole isomers. The difference in profile between the 1,2,4 and 1,3,4 regioisomers can be rationalized by their intrinsically different charge distributions (e.g., dipole moments). To facilitate the use of these heteroaromatic rings, novel synthetic routes for ready access of a broad spectrum of 1,3,4-oxadiazoles, under mild conditions, are described.

17O NMR studies of substituted 1,3,4-oxadiazoles

Three series of substituted 1,3,4-oxadiazoles were studied by 17O NMR spectroscopy. Chemical shifts values were correlated with empirical Hammett parameters as well as calculated bond lengths and chemical shielding values.

Microwave assisted syntheses of 2,5-disubstituted 1,3,4-oxadiazoles

2,5-Di-substituted 1,3,4-oxadiazoles have been synthesized from the oxidation of 1-aroyl-2-arylidene hydrazines with potassium permanganate on the surface of solid mineral support as well as in the mixture of acetone and water under microwave irradiation. 2,5-Disubstituted 1,3,4-oxadiazoles have been synthesized by oxidation of 1-aroyl-2-arylidene hydrazines with potassium permanganate on the surface of a solid mineral support as well as in mixtures of acetone and water under microwave irradiation.

APO AI EXPRESSION ACCELERATING AGENT

Pharmaceutical compositions for enhancing the expression of apoAI are provided.Pharmaceutical compositions for enhancing the expression of apoAI which comprises a compound of formula (I): in which Y1 is O, S or NR1; Y2, Y

TETRAZOLES IN THE SYNTHESES OF 1,3,4-OXADIAZOLES

Various variants of cleavage of tetrazoles to form 1,3,4-oxadiazoles are examined.The mechanisms and synthetic potentialities of these reactions are discussed.

Studies on Thioamides and Their Derivatives,VI. New Synthesis of 5-Membered Heterocyclic Compounds

Simple N-monosubstituted thioamides react with acid hydrazides to form 1,2,4-triazole derivatives.N,N-Disubstituted thioamides alkylated with methyl iodide readily yield with acid hydrazides 1,3,4-oxadiazoles.

Research in the 2,5-Diaryl-1,3,4-oxadiazole Series. 1. Electronic Structures and Spectral-Luminescence Properties of Substituted 2,5-Diphenyl-1,3,4-oxadiazoles

The dependence of the spectral-luminescence properties of substituted 2,5-diphenyl-1,3,4-oxadiazoles on the electronic nature of the substituents was studied.Experimental and theoretical studies confirm the electron-acceptor character of the oxadiazole ring and constitute evidence for the rather effective transmission of the electronic effects through the heteroring.