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Classical oxazole synthetic methods in organic chemistry are

Synthesis of benzoxazole- . The synthesis comprises four steps and an overall yield of 3.

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Benzoxazole and Benzothiazole Synthesis ..

A series of new compounds containing a benzimidazole, benzothiazole, or benzoxazole nucleus linked to an arylpiperazine by different thioalkyl chains was prepared. They were tested in radioligand binding experiments to evaluate their affinity for 5-HT1A and 5-HT2A serotonergic, α1 adrenergic, D1, and D2 dopaminergic receptors. Many of tested compounds showed an interesting binding profile; in particular, 36 displayed very high 5-HT1A receptor affinity and selectivity over all the other investigated receptors. Selected compounds, evaluated in functional assays, showed antagonistic or partial agonistic activity at 5-HT1A receptor. An extensive conformational research using both NMR and modeling techniques indicated that extended conformations predominated in vacuum, in solution and during interactions with 5-HT 1A receptor. Finally, the elaborated binding mode of selected compounds at 5-HT1A receptor was used to explain the influence of spacer length on ligands affinity.

A small library of achiral 4-hydroxybenzoxazoles were synthesised in good yields.

N2 - A series of new compounds containing a benzimidazole, benzothiazole, or benzoxazole nucleus linked to an arylpiperazine by different thioalkyl chains was prepared. They were tested in radioligand binding experiments to evaluate their affinity for 5-HT1A and 5-HT2A serotonergic, α1 adrenergic, D1, and D2 dopaminergic receptors. Many of tested compounds showed an interesting binding profile; in particular, 36 displayed very high 5-HT1A receptor affinity and selectivity over all the other investigated receptors. Selected compounds, evaluated in functional assays, showed antagonistic or partial agonistic activity at 5-HT1A receptor. An extensive conformational research using both NMR and modeling techniques indicated that extended conformations predominated in vacuum, in solution and during interactions with 5-HT 1A receptor. Finally, the elaborated binding mode of selected compounds at 5-HT1A receptor was used to explain the influence of spacer length on ligands affinity.

China Synthesis of the Benzoxazole Compound …

Synthesis of some novel benzoxazole derivatives and their antimicrobial activity

Benzoxazole and Benzothiazole Synthesis from Carboxylic Acids in Solution and on Resin by Using Ethyl 2-Cyano-2-(2-& &. Synthesis and properties of hyperbranched polyurethanes. Synthesis of AB-type block copolymers containing benzoxazole and anthracene groups by ATRP and fluorescent property. Standard PDF (344.5 kB). Synthesis and characterization of oxazolopyridine and benzoxazole derivatives Venkatachalam.

T1 - Synthesis of new arylpiperazinylalkylthiobenzimidazole, benzothiazole, or benzoxazole derivatives as potent and selective 5-HT1A serotonin receptor ligands

Synthesis and evaluation of anticancer benzoxazoles …

01/01/2018 · Synthesis, characterization and biological evaluation of benzoxazole ..

The total synthesis of the spiroketal ionophore antibiotic routiennocin 1 (CP-61,405) employing π-allyltricarbonyl iron lactone complexes is described. These complexes were used as precursors for the preparation of substituted 2-phenylsulphonyl pyrans which, in turn, were coupled with iodoacetonides to afford spiroketals. Elaboration of the spiroketals by tetra-n-propylammonium perruthenate (TPAP) oxidation and coupling with 2-lithio-1-[β-(trimethylsilyl)ethoxymethyl] pyrrole followed by further oxidation, deprotection, oxidation and benzoxazole formation afforded the natural product. The preparation of the amino phenol fragment necessary for benzoxazole formation involved a novel amination procedure using benzeneselenenic anhydride and hexamethyldisilazane followed by samarium diiodide reduction.

N2 - The total synthesis of the spiroketal ionophore antibiotic routiennocin 1 (CP-61,405) employing π-allyltricarbonyl iron lactone complexes is described. These complexes were used as precursors for the preparation of substituted 2-phenylsulphonyl pyrans which, in turn, were coupled with iodoacetonides to afford spiroketals. Elaboration of the spiroketals by tetra-n-propylammonium perruthenate (TPAP) oxidation and coupling with 2-lithio-1-[β-(trimethylsilyl)ethoxymethyl] pyrrole followed by further oxidation, deprotection, oxidation and benzoxazole formation afforded the natural product. The preparation of the amino phenol fragment necessary for benzoxazole formation involved a novel amination procedure using benzeneselenenic anhydride and hexamethyldisilazane followed by samarium diiodide reduction.

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  • Studies in the synthesis of benzoxazole compounds

    Synthesis, Anti-Breast Cancer Activity and Molecular Modeling of Some Benzothiazole and Benzoxazole Derivatives

  • "Synthesis and coordination chemistry of new oxazoline …

    Application of SBA-Pr-SO3H in the synthesis of benzoxazole derivatives

  • investigated the synthesis of 2, 5, 6-substituted benzoxazole …

    Synthesis and properties of polyimides-containing benzoxazole units in the main chain

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Direct Synthesis of Photosensitive Poly(benzoxazole)

Finally a small library of chiral benzoxazoles and 4-hydroxybenzoxazoles were synthesised,starting from amino acids and utilising a Mitsunobu reaction to perform the ring closing.

Synthesis of arylamines - Organic Chemistry Portal

In this thesis it was attempted to investigate the synthesis, functionalisationand coordination chemistry of these compound class and finally look at a method ofsynthesising chiral 4-hydroxybenzoxazoles from amino acids.

Research & Development Chemicals

Herein method for the synthesis of substituted 1,2-benzoxazolone (8a-f) and 3-chloro-1,2-benzoxazole (9a-f) derivatives has been described. A new scheme has been adapted for the construction of 1,2-benzoxazole ring from salicylic acid and its derivatives which leads to the formation of series of 5,6 and 7 substituted title compounds. Synthesized compounds were characterized by IR, 1H-NMR and Mass spectral analysis. Spectral data confirmed the compounds formation. Final compounds (8a-f) and (9a-f) were screened for their in-vivo analgesic activity by acetic acid induced writhing method in rats and anti-inflammatory activity by carrageenan-induced paw edema model. Among the compounds screened compound 8a and compound 9c showed good analgesic activity of about 45% (writhing mean 8.9) and 54% (writhing mean 7.5) inhibition respectively at 5 mg/Kg po dosage. Compounds 8b and 9b (both having inhibition edema of 66.1%) showed significant anti-inflammatory activity. Other derivatives exhibit moderate to good analgesic and anti-inflammatory activities.

Also available following 2-Mercapto Benzimidazole derivatives

AB - A series of new compounds containing a benzimidazole, benzothiazole, or benzoxazole nucleus linked to an arylpiperazine by different thioalkyl chains was prepared. They were tested in radioligand binding experiments to evaluate their affinity for 5-HT1A and 5-HT2A serotonergic, α1 adrenergic, D1, and D2 dopaminergic receptors. Many of tested compounds showed an interesting binding profile; in particular, 36 displayed very high 5-HT1A receptor affinity and selectivity over all the other investigated receptors. Selected compounds, evaluated in functional assays, showed antagonistic or partial agonistic activity at 5-HT1A receptor. An extensive conformational research using both NMR and modeling techniques indicated that extended conformations predominated in vacuum, in solution and during interactions with 5-HT 1A receptor. Finally, the elaborated binding mode of selected compounds at 5-HT1A receptor was used to explain the influence of spacer length on ligands affinity.

PDF Downloads : Oriental Journal of Chemistry

AB - The total synthesis of the spiroketal ionophore antibiotic routiennocin 1 (CP-61,405) employing π-allyltricarbonyl iron lactone complexes is described. These complexes were used as precursors for the preparation of substituted 2-phenylsulphonyl pyrans which, in turn, were coupled with iodoacetonides to afford spiroketals. Elaboration of the spiroketals by tetra-n-propylammonium perruthenate (TPAP) oxidation and coupling with 2-lithio-1-[β-(trimethylsilyl)ethoxymethyl] pyrrole followed by further oxidation, deprotection, oxidation and benzoxazole formation afforded the natural product. The preparation of the amino phenol fragment necessary for benzoxazole formation involved a novel amination procedure using benzeneselenenic anhydride and hexamethyldisilazane followed by samarium diiodide reduction.

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