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A novel tert-butoxycarbonylation reagent: 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI)

The use of 1-tert-butoxy-2-tert-butoxycarbonyl-1,2-dihydroisoquinoline (BBDI) as a tert-butoxycarbonylation reagent for acidic proton-containing substrates such as phenols, aromatic and aliphatic amines hydrochlorides, and aromatic carboxylic acids in the absence of a base is described. The reactions proceed chemoselectively in high yield under mild conditions.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N383 – PubChem

Awesome and Easy Science Experiments about Phthalazine

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253-52-1, Name is Phthalazine, belongs to phthalazine compound, is a common compound. COA of Formula: C8H6N2In an article, once mentioned the new application about 253-52-1.

Mono- and heteroligand iron(II) complexes with tris(3,5-dimethylpyrazol-1-yl)methane

Coordination compounds of iron(II) thiocyanate with tris(3,5-dimethylpyrazol-1-yl)methane (HC(3,5-Me2Pz)3), [Fe(HC(3,5-Me2Pz)3)2](NCS)2] (I) and [Fe(HC(3,5-Me2Pz)3)(?hz)(NCS)2] ¡¤ H2O (II), where ?hz is phthalazine, are synthesized. The complexes are studied by X-ray diffraction analysis, diffuse reflectance and IR spectroscopy, and static magnetic susceptibility measurements. The single crystals are obtained, and the molecular and crystal structures of complex II and compounds [Fe(HC(3,5-Me2Pz)3)(3,5-Me2Pz)(NCS)2] ¡¤ ?2H5OH (III), where 3,5-Me2Pz is 3,5-dimethylpyrazole, and [Fe(HC(3,5-Me2Pz)3)2][Fe(HC(3,5-Me2Pz)3)(NCS)3]2 (IV) are determined (CIF files CCDC 1415452 (II), 1415453 (III), and 1415454 (IV)). The study of the temperature dependence mueff(?) in a range of 2?300 K shows exchange interactions of the antiferromagnetic character between the iron(II) ions in complexes I and II.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N248 – PubChem

Final Thoughts on Chemistry for Phthalazine

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Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review

Phthalazine, a structurally and pharmacologically versatile nitrogen-containing heterocycle, has gained more attention from medicinal chemists in the design and synthesis of novel drugs owing to its pharmacological potential. In particular, phthalazine scaffold appeared as a pharmacophoric feature numerous drugs exhibiting pharmacological activities, in particular, antidiabetic, anticancer, antihypertensive, antithrombotic, anti-inflammatory, analgesic, antidepressant and antimicrobial activities. This review presents a summary of updated and detailed information on phthalazine as illustrated in both patented and non-patented literature. The reported literature have described the optimal pharmacological characteristics of phthalazine derivatives and highlighted the applicability of phthalazine, as potent scaffold in drug discovery.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N386 – PubChem

Awesome and Easy Science Experiments about Phthalazine

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Microwave assisted synthesis of six member ring azaheterocycles and their antimycobacterial and anticancer evaluation

We report herein a comparative study concerning the influence of microwave (MW) irradiation comparative with conventional thermal heating (TH) in the reaction of six member ring azaheterocycles (derived from phenanthroline, quinoline, isoquinoline and phthalazine) with ethyl cyanoformate, and their anticancer and antimycobacterial activity. Under MW irradiation the reactions have some undeniable advantages: the reaction times decrease dramatically (from hours to minutes), the yields are higher, the reactions became selective in some cases (4,7-phenanthrolinium and phthalazinium ylides). The decreasing of reaction time+ from hours to minutes corroborated with the fact that in majority of cases the yield are higher and the selectivity is better, allow us to say that these reactions could be considered as eco-friendly. As far for biological activity, three of the compounds exhibited a significant antitumor activity against some cancer cell lines including prostate cancer, leukemia, renal cancer, lung cancer and breast cancer. The best potency in terms of growth inhibition of tumor cells (~45%) was shown by compound 4a against renal cancer A498 and ovarian cancer SK-OV-3 cells. The tested compounds have not shown any antimycobacterial activity against Mycobacterium tuberculosis.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N28 – PubChem

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 253-52-1, and how the biochemistry of the body works.Computed Properties of C8H6N2

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 253-52-1, name is Phthalazine, introducing its new discovery. Computed Properties of C8H6N2

A New Entry to the Ethynylation of Azaaromatics Using Bis(tributylstannyl)acetylene in the Presence of Alkyl chloroformate

Unstable N-alkoxycarbonyl quaternary salts of azaaromatics were trapped in situ by bis(tributylstannyl)acetylene followed by the treatment with trifluoroacetic acid to give 2-ethynyl adducts in good yields.The same compounds were obtained only in low yields when ethynyltributyltin was used as a nucleophile.The reaction was revealed to be available for various aromatics including pyridine, pyrazine, imidazole, thiazole, oxazole, and benzodiazines.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N204 – PubChem

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Polyoxometalate Photocatalysis for Liquid-Phase Selective Organic Functional Group Transformations

Polyoxometalates (POMs), which are anionic metal oxide clusters, have recently attracted considerable attention as photocatalysts because of their unique photoinduced charge-transfer properties, redox properties, acid-base properties, and reactivities. In this Review, we present a summary of recent developments in POM photocatalysis for organic synthesis. Various organic functional group transformations can be selectively induced by photoirradiation in the presence of catalytic amounts of suitably designed POMs. In particular, many liquid-phase functional group transformations based on the activation of substrates by decatungstate have been reported. However, decatungstate photocatalysis requires irradiation with UV light because of the large energy gaps between the O2–based highest occupied molecular orbitals (HOMOs) and the W6+-based lowest unoccupied molecular orbitals (LUMOs) therein. Various strategies have been developed in efforts to utilize visible light, including hybridization with photosensitizers, metal substitution, and coordination of ligands (substrates) at the vacant sites of lacunary POMs. We also present here an overview of our recent work on the development of visible-light-responsive POM catalysts by HOMO- and LUMO-engineering strategies for both the oxidation and reduction of organic substrates, including amines, alcohols, nitroarenes, sulfides, sulfoxides, and pyridine N-oxides.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N430 – PubChem

Brief introduction of Phthalazine

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Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer

Herein we report the synthesis of two series of 4-phenylphthalazin-1-ones 11a-i and 4- benzylphthalazin-1-ones 16a-h as anti-lung adenocarcinoma agents with potential inhibitory activity against PARP-1. All the newly synthesized phthalazinones were evaluated for their anti-proliferative activity against A549 lung carcinoma cell line. Phthalazinones 11c-i and 16b, c showed significant cytotoxic activity against A549 cells at different concentrations (0.1, 1 and 10 muM) for two time intervals (24 h and 48 h). These nine phthalazinones were further examined for their inhibitory activity towards PARP-1. Compound 11c emerged as the most potent PARP-1 inhibitor with IC50 value of 97 nM, compared to that of Olaparib (IC50 = 139 nM). Furthermore, all these nine phthalazinones passed the filters of Lipinski and Veber rules, and predicted to have good pharmacokinetics properties in a theoretical kinetic study. On the other hand, western blotting in A549 cells revealed the enhanced expression of the cleaved PARP-1, alongside, with the reduced expression of pro-caspase-3 and phosphorylated AKT. In addition, ELISA assay confirmed the up-regulation of active caspase-3 and caspase-9 levels compared to the control, suggesting the activation of the apoptotic machinery in the A549 cells. Finally, molecular docking of 11c into PARP-1 active site (PDB: 5WRZ) was performed to explore the probable binding mode.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N32 – PubChem

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Luminescent dinuclear rhenium(I) complexes containing bridging 1,2-diazine ligands: Photophysical properties and application

In this contribution we provide an overview of the preparation and of the properties of different classes of luminescent dinuclear tricarbonyl rhenium(I) complexes of general formula [Re2(mu-X)2(CO)6(mu-1,2-diazine)] (X=halide, hydride, alkoxide, and thiolate). Their electrochemical and photophysical properties in solution are presented, as well as combined density functional (DFT) and time-dependent density functional (TDDFT) studies of their geometry, relative stability and electronic structure. The relationships between the structure and the emission properties of the complexes are discussed in detail, showing a modulation effect of the bridging ancillary ligands as well as of the diazine substituents on energy, lifetime and quantum yield of the emission. Photoluminescent quantum yields (Phi) up to 0.53 have been measured in fluid solution for the dichloro complexes containing diazines bearing alkyl groups in both the beta positions, designed to optimize all the parameters responsible for the radiative decay. The photophysical properties in the solid state are also briefly presented, showing in some cases an increase of the emission intensity, discussed in terms of restriction of intramolecular roto-vibrational motions. These properties, together with their good processability and high stability, allowed the successful use of some of these complexes as a phosphorescent dopant in OLEDs. The good performances of OLED devices prepared both by solution- and vacuum-processing are reported. The preliminary work exploring the potential of these complexes as luminescent labels for bioimaging is also presented.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N332 – PubChem

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Spiroheterocyclic compounds: old stories with new outcomes

An efficient and straightforward method for the preparation of spirodiazine derivatives is reported which involves mild reaction conditions and easily accessible reactants. A new class of spiroazaheterocycles, spiro[pyrrolidine-pyrrolo[3,4-c]pyrroles], is obtained. A feasible explanation is given for the unexpected results obtained at high energy (high temperatures, MW and ultrasound irradiation).

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N292 – PubChem

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Aldehyde oxidase 1 (AOX1) in human liver cytosols: Quantitative characterization of AOX1 expression level and activity relationships

Aldehyde oxidase 1 (AOX1) is a cytosolic enzyme highly expressed in liver and plays a key role in metabolizing drugs containing aromatic azaheterocyclic substituents. Rapid metabolism catalyzed by AOX1 can cause a drug to exhibit high clearance, low exposure, and hence decreased efficacy or even increased toxicity (if AOX1 generated metabolites are toxic). There is a need to develop the correlation between AOX1 expression levels and AOX1-substrate clearance. A fast, sensitive, and robust liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed to quantify AOX1 in human liver cytosol for the first time. This LC-MS/MS method includes a straightforward ultrafiltration fractionation step and gives great selectivity and wide dynamic range (5.2 pM to 20.7 nM). The AOX1 levels in human liver cytosols of 20 donors were quantified using this method to investigate individual differences in AOX1 expression. No significant individual or gender differences in AOX1 levels were observed, although male donors exhibited a broader distribution than female donors (0.74-2.30 pmol/mg versus 0.74-1.69 pmol/mg, respectively). The AOX1 protein levels measured by LC-MS/MS were consistent with those measured by an enzyme-linked immunosorbent assay. Several donors have a normal AOX1 protein level but low enzyme activity, which might be due to cofactor deficiency, single nucleotide polymorphism, or homodimer dissociation. Cytosols from donors with chronic alcohol consumption had low AOX1-catalyzed carbazeran oxidation activities (<51 mul/min per milligram compared with a median of 455 mul/min per milligram), but preserved similar AOX1 protein expression levels (approximately 15% less than the median value). Copyright Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. category: phthalazine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 253-52-1, in my other articles.

Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N156 – PubChem