59918-86-4

Upstream product

• 1641-09-4 3-thiophenecarbonitrile 
• 498-62-4 3-thiophene carboxaldehyde 
• 54610-58-1 ethyl thiophene-3-carbimidate hydrocloride 

Downstream Products

• 1073313-90-2 5-(2-(4-biphenylyl)thiophen-3-yl)-2-trityl-2H-tetrazole 
• 1073313-93-5 5-(2-(naphthalen-1-yl)thiophen-3-yl)-2-trityl-2H-tetrazole 
• 1073314-21-2 (E)-3-(3-((5-((E)-2-carboxyvinyl)-3-(1H-tetrazol-5-yl)thiophen-2-yl)methyl)phenyl)acrylic acid 
• 1073314-15-4 (E)-3-(5-benzyl-4-(2-(2-carboxyethyl)-2H-tetrazol-5-yl)thiophen-2-yl)acrylic acid 
• 1073314-14-3 (E)-methyl 3-(5-benzyl-4-(2-(3-methoxy-3-oxopropyl)-2H-tetrazol-5-yl)thiophen-2-yl)acrylate 
• 1073313-84-4 (E)-methyl 3-(5-benzyl-4-(2-methyl-2H-tetrazol-5-yl)thiophen-2-yl)acrylate 
• 1073313-83-3 (E)-methyl 3-(5-benzyl-4-(1-methyl-1H-tetrazol-5-yl)thiophen-2-yl)acrylate 
• 1073313-80-0 (E)-methyl 3-(5-benzyl-4-(1H-tetrazol-5-yl)thiophen-2-yl)acrylate 
• 1073313-79-7 (Z)-methyl 3-(5-benzyl-4-(1H-tetrazol-5-yl)thiophen-2-yl)acrylate 
• 1073314-17-6 2-benzhydryl-5-(2-bromothiophen-3-yl)-2H-tetrazole 
• 908588-12-5 5-(2-(tributylstannyl)thiophen-3-yl)-2-trityl-2H-tetrazole 
• 908588-13-6 5-(2-benzylthiophen-3-yl)-2-trityl-2H-tetrazole 
• 908588-09-0 5-(thiophen-3-yl)-2-trityl-2H-tetrazole 

Relevant academic research and scientific papers

Highly active and reusable cu/c catalyst for synthesis of 5-substituted 1h-tetrazoles starting from aromatic aldehydes

A new, efficient and convenient method for the synthesis of 5-substituted 1H-tetrazole derivatives with a wide range of substituents in good to excellent yields has been developed. The synthesis was performed by the one-pot three-component [3+2]cycloaddit

Antibacterial assessment of heteroaryl, Vinyl, Benzyl, and Alkyl tetrazole compounds

Background: In previous reports, the antibacterial properties of certain tetrazole derivatives have been described. We have previously reported the antibacterial properties of aryl 1H-tetrazole compounds. Objective: To study the antibacterial activity of 5-substituted heteroaryl, vinyl, benzyl, and alkyl 1H-tetrazole derivatives. Methods: The antibacterial properties of heteroaryl, vinyl, benzylic, and aliphatic tetrazole derivatives were investigated against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The activity was assessed by determining the minimum inhibitory concentration of these tetrazole derivatives and comparing them to the known antibiotics amoxicillin, trimethoprim and sulfamethoxazole. Results: The tetrazole compounds were prepared utilizing cerium(III) chloride heptahydrate catalysis at 160o C for 1-4 h in a microwave reactor using an aqueous solvent mixture. The most active derivatives exhibited minimum inhibitory concentration values between 125-250 μg/mL against Escherichia coli. More importantly, these compounds were considerably more active when used in combination with trimethoprim and a significant synergistic effect was observed (MIC = 0.98-7.81 μg/mL) against E. coli and S. aureus. Conclusion: The tetrazole derivatives were synthesized in high yield and short reaction times in water. Several of the tetrazole compounds showed a significant synergistic antibacterial effect when used with trimethoprim.

Preparation of 5-substituted 1H-tetrazoles catalyzed by scandium triflate in water

Several 5-substituted 1H-tetrazoles were prepared in water or isopropanol/water mixtures using microwave heating. Good yields were obtained for the [2 + 3] cycloaddition of sodium azide with aryl nitriles, aliphatic nitriles, and vinyl nitriles when catal

Microwave Synthesis of 5-Substituted 1 H-Tetrazoles Catalyzed by Bismuth Chloride in Water

(Chemical Equation Presented). Bismuth chloride was used to catalyze the [2 + 3] cycloaddition between sodium azide with aryl nitriles, aliphatic nitriles, and vinyl nitriles. A number of 5-substituted 1H-tetrazoles were synthesized in water or isopropano

CuFe2O4 nanoparticles: A magnetically recoverable and reusable catalyst for the synthesis of 5-substituted 1H-tetrazoles

An efficient and economical protocol for the synthesis of 5-substituted 1H-tetrazoles from various nitriles and sodium azide is described using magnetically recoverable and reusable CuFe2O4 nanoparticles. A wide variety of aryl nitriles underwent [2+3] cycloaddition under mild reaction conditions to afford tetrazoles in good to excellent yields. The catalyst was magnetically separated and reused five times without significant loss of catalytic activity.

Iron salts in the catalyzed synthesis of 5-substituted 1H-tetrazoles

A study was conducted to investigate the presence of iron salts in the catalyzed synthesis of 5-substituted 1H-tetrazoles. Para-trifluorotoluonitrile and trimethylsilyl azide were selected as model substrates for the initial metal source screening and the optimization of the reaction conditions. It was observed that the catalysis proceeded successfully producing tetrazole in 91% yield. A screening of various iron salts revealed that both the oxidation state of the iron and the counterion had a minor effect on the catalysis. Iron sources with different purity grades obtained from various providers were applied to investigate that the catalysis was not resulting from trace impurities in the metal salt. It was also observed that the catalysis proceeded successfully for a wide variety of aryl nitriles, providing tetrazoles in high yields. The best catalysis results were achieved with compounds that contained electron-withdrawing groups.

THERAPEUTIC PRO-ANTIBIOTIC AGENTS AND METHODS OF USE THEREOF

The present invention provides for therapies characterized in part by co-administration or combination of antibiotic agents with medicinal compositions comprising as the pro-antibiotic active ingredient either a compound represented by a formula [I] or a

DESIGN AND SYNTHESIS OF NOVEL ANTIMICROBIALS

The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable bin

Fast microwave-assisted preparation of aryl and vinyl nitriles and the corresponding tetrazoles from organo-halides

Aryl and vinyl nitriles have been prepared in very high yields from the corresponding bromides using palladium-catalyzed reactions with microwave irradiation employed as the energy source. Furthermore, flash heating was used successfully for the conversion of these nitriles into aryl and vinyl tetrazoles by cycloaddition reactions. One-pot transformation of aryl halides directly to the aryl tetrazoles could be accomplished both in solution and on solid support. All reactions were completed in minutes rather than in hours or days as previously reported with the standard thermal heating technique. A very potent HIV-1 protease inhibitor (K(i) = 0.56 nM), comprising two tetrazole heterocycles as carboxyl group bioisosteres, was prepared in one pot by microwave-promoted cyanation of a bromo precursor and a subsequent cycloaddition reaction. The temperature-time profiles at 13, 20, and 60 W magnetron input power in DMF are presented.