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Radical Decarboxylative Alkylation onto Heteroaromatic Bases with Trivalent Iodine Compounds

Heteroaromatic bases containing nitrogen atoms were easily alkylated with carboxylic acids in the presence of benzene and pentafluorobenzene via radical pathways.Similarly, the alkylation onto heteroaromatic bases was carried out with oxalic acid monoalkyl esters, which were prepared from alcohols and oxalyl dichloride, in the presence of the same trivalent iodine compounds.Moreover, this system was applied to the synthesis of C-nucleosides with the carboxylic acids bearing a sugar moiety.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N447 – PubChem

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Dioxygenation of alkenes

A plethora of natural products exist that contain characteristic vicinal 1,2-diols in their scaffolds. The alkene dihydroxylation methodology developed by Sharpless continues to be the most robust and general method to obtain this important motif. However, the main problem with this transformation is the use of osmium as the catalyst and, since the 1990s, various methods have been developed that employ alternative transition metals. In this chapter, the most important protocols for the racemic and enantioselective dioxygenation of alkenes mediated by metals are summarized, together with recently developed methods that employ chiral nonracemic hypervalent iodine(III) reagents.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N280 – PubChem

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Direct Electron Paramagnetic Resonance Observation of Strong Vibronic mixing in a Nonphosphorescent Triplet State. Phthalazine in a Biphenyl Host

The lowest excited triplet state of nonphosphorescent phthalazine was investigated by the time-resolved EPR technique.The hyperfine structure and the angular dependence of the signals observed at 4.2 K in a biphenyl host give rise to very unusual EPR parameters which lead to the conclusion that the T1 state is a heavily mixed state of n?* and ??* character.The lack of phosphorescence is discussed on the basis of the obtained results.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N443 – PubChem

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Tropical and Subtropical Parasitic Diseases: Targets for a New Approach to Virtual Screening

Computational techniques are widely used to reduce costs associated with new drug development with the ability to bind a specific molecular target. These studies need a Brookhaven protein data bank structure sample of the enzyme interaction with an inhibitor of adequate size. In this context, a new computational methodology is postulated to be used when there are no published samples fulfilling this requirements. In this study, 7 compounds, which showed anti-T. cruzi, L. donovani and L. infantum properties, and proved to be inhibitors of their Fe-SOD enzymes, have been theoretically evaluated against related parasites Fe-SOD enzymes, which have been proposed as targets for antiparasitic drugs. This methodology may be applied to similar cases and also to generate starting structures to be used with different CADD methods.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N497 – PubChem

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An overview of aldehyde oxidase: an enzyme of emerging importance in novel drug discovery

Introduction: Given the rising trend in medicinal chemistry strategy to reduce cytochrome P450-dependent metabolism, aldehyde oxidase (AOX) has recently gained increased attention in drug discovery programs and the number of drug candidates that are metabolized by AOX is steadily growing. Areas covered: Despite the emerging importance of AOX in drug discovery, there are certain major recognized problems associated with AOX-mediated metabolism of drugs. Intra- and inter-species variations in AOX activity, the lack of reliable and predictive animal models using the common experimental animals, and failure in the predictions of in vivo metabolic activity of AOX using traditional in vitro methods are among these issues that are covered in this article. A comprehensive review of computational human AOX (hAOX) related studies are also provided. Expert opinion: Following the recent progress in the stem cell field, the authors recommend the application of organoids technology as an effective tool to solve the fundamental problems associated with the evaluation of AOX in drug discovery. The recent success in resolving the hAOX crystal structure can too be another valuable data source for the study of AOX-catalyzed metabolism of new drug candidates, using computer-aided drug discovery methods.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N358 – PubChem

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Fused azole-thiazolines: Via one-pot cyclization of functionalized N-heterocyclic carbene precursors

A one-pot two-step methodology was exploited to synthesize fused thiazoline-azolium salts via reactions of bromoalkyl-azolium salts with KSCN and NaOH. The synthetic feasibility and versatility was demonstrated by the high yield (>80%) preparation of 13 salts with different backbones, linkers and substituents. Using methylpropionato as an N-protecting group, the resulting salts could be further derivatized to their neutral azole-thiazolines. The reaction sequence proceeds via (i) Br ? SCN substitution, (ii) N-heterocyclic carbene formation, (iii) carbene attack of the S atom and CN- displacement in the alkyl-S-CN unit, and (iv) methyl acrylate elimination.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N439 – PubChem

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Surface enhanced Raman scattering of benzotriazole: A molecular orientational study

Surface enhanced Raman scattering of benzotriazole in aqueous silver sol at pH ?9 has been investigated. The spectra of the molecule at various concentrations were recorded and the maximum enhancement was observed with a 10-5 M solution. From the comparison of the surface enhanced Raman spectra with the conventional Raman spectra and applying ‘surface selection rule’, it is inferred that the molecular ion interacts with the silver sol via the nitrogen atoms of the benzotriazole ring and the molecule assumes a near ‘end-on’ orientation.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N445 – PubChem

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4-Piperidinecarboxamide modulators of vanilloid VR1 receptor

This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N6 – PubChem

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Some Reactions of N-Alkoxycarbonyl Reissert Compounds with Heterocumulenes: Formation of the Imidazo<5,1-a>isoquinoline and Imidazo<5,1-a>phthalazine Systems and Related Chemistry

Chloroformate derived Reissert compounds of isoquinoline and of phenanthridine on treatment with base undergo cyclisation with isothiocyanates to give in good yields corresponding imidazo<5,1-a>isoquinoline and imidazo<1,5-f>phenanthroline derivatives.Phthalazine Reissert compound analogues give open chain adducts under the same conditions which can be cyclised to derivatives of the novel imidazo<5,1-a>phthalazine system by heating in the presence of molecular sieves.When carbon disulphide is the heterocumulene cyclisation is not observed but open chain dithio-ester derivatives can be isolated on alkylation of the intermediate sodium salts.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N453 – PubChem

A new application about Phthalazine

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A spectrophotometric method for the determination of aldehyde oxidase activity using 3-methyl-2-benzothiazolinone hydrazine: A preliminary study

Aldehyde oxidase, a molybdenum cofactor-containing cytosolic enzyme, is extensively distributed throughout the animal kingdom. The enzyme is mainly active in liver and other tissues of mammalian species and involved in the metabolism of wide range of aldehydes and nitrogen-containing molecules. A continuous spectrophotometric method for the quantitative determination of aldehyde oxidase, AO, enzyme activity is described in this article. This method is based on the coupling reaction between 3-methyl-2-benzothiazolinone hydrazone (MBTH) and the o-quinone. Dopamine as substrate for AO, is converted/oxidized to o-quinone. The latter react with MBTH to produce intensely colored products that absorb light maximally in the visible region. Then, AO activity has been kinetically characterized; the Km (Michaelis-Menten constant) and Vmax (maximum initial velocity) values for the oxidation of dopamine by AO were evaluated. The existence of MBTH in the reaction medium and production of stable color as well as the high epsilon values at 510 nm of MBTH-Q adduct make this direct technique more sensitive than other continuous methods for AO assay. The optimized MBTH reaction may be useful for biological staining of AO activity isolated from various biological sources in electrophoresis gels.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N410 – PubChem