throughput synthesis of benzimidazoles.

To synthesize NHCs, the more common practice is substitutions of alkyl/aryl groups at nitrogens of azoles (imidazole, benzimidazole, triazole etc.) to synthesize azolium salts in which H-2 hydrogen becomes acidic which can be removed by addition of a base (e.g., t-BuOK, NaH etc.)[,]. There are numerous ways to generate free NHCs and their metal complexes[,].

Synthesis of 2-Mercaptobenzoxazoles and 2-Mercaptobenzimidazole ..

This chapter focuses on the methods of preparation of imidazoles and benzimidazoles with a ..
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of benzimidazoles in dry medium.

A wide variety of heterocyclic compounds based on imidazole, benzimidazole, pyrimidine, pyridine and purine are being intensively studied as anticancer agents against various cancer cell lines[,]. Furthermore, imidazole and benzimidazole-based compounds appear to be very promising candidates for anticancer treatment. As reported in recent reviews there has been a growing interest in the community of synthetic organic chemistry to examine the anticancer activities of different heterocyclic compounds with specific functional groups[]. In this perspective, we have designed a series of bis-benzimidazolium salts with different counter ions.

12/04/2012 · Synthesis of N-alkyl benzimidazoles ..

In conclusion, a series of bis-benzimidazolium salts was prepared in two steps. First, the preparation of N-alkyl benzimidazoles by the reaction of benzimidazole with appropriate alkyl halide in presence of potassium hydroxide. Second, the subsequent treatment of N-alkyl benzimidazole derivatives with 1,3-dibromomethylbenzene in 1,4-dioxane at refluxing temperature afforded the title compounds in good yields. Structures of selected salts were established through single crystal X-ray diffraction technique. All the synthesized salts were applied against human colon cancer cell line which showed dose-dependent cytotoxicity. Furthermore, the compounds with either bromide anion or N-methylene phenyl and N-heptyl substitutions found to be more potent cytotoxic. Thus, studies on the synthesis of respective silver complexes to observe the change in activity against human colorectal cancer cell line are in progress.

Lopez JE, Guadalupe G, Alvarez CT (2000) Synthesis of benzimidazoles in dry medium.
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Oxone, Potassium peroxomonosulfate - Organic …

ABSTRACT: A survey of green synthesis of thiazines and oxazines revealed the moiety have attracted a great deal of interest of medicinal chemist, biochemist, pharmacologist and rendered as a lead molecule for designing potential bioactive agents. This review accompanying supplementary green synthetic information & its references would extend great deal of help to researchers in determining the best and most productive, economical, suggestive and clinically important compound of thiazine and oxazine derivatives which will be expected to show potent pharmacological activities. This has led to the discovery of a wide variety of compounds that are of high interest from the point of view antimicrobial, antimycobacterial, antidiabetic and antidepressant effects among others.

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In conclusion, we have synthesized successfully a series of novel benzimidazole derivatives with good antimycobacterial properties against M. tuberculosis. Encouraged by the positive results we have reported here, further modification on the 4-position on the bisulfite adducts as well as quantitative structure-activity relationship (QSAR) is currently in progress in our laboratory. It is conceivable that derivatives showing antimycobacterial activity can be further modified to exhibit better potency than standard drugs.

Parallel and automated library synthesis of ..

A number of N-alkylbenzimidazoles were synthesized by reactions of benzimidazole with alkyl halides (i-PrBr, PrBr, EthBr, Pent-2-ylBr, BuBr, BenzCl, HeptBr). The subsequent treatment of the resulting N-alkylbenzimidazoles with 1,3-(bromomethylene)benzene afforded corresponding bis-benzimidazolium salts. All synthesized compounds were characterized by spectroscopic techniques (Additional file: NMR & FT-IR) and microanalysis. Molecular structures of selected compounds were established through single crystal x-ray diffraction studies. All the compounds were assessed for their anti-proliferation test on human colorectal cancer cell line (HCT 116). Results showed that the compounds exhibited dose dependent cytotoxicity towards the colon cancer cells with IC50 ranges between 0.1 to 17.6 μM. The anti-proliferation activity of all compounds was more pronounced than that of standard reference drug 5-flourouracil (IC50 =19.2 μM).