Category: 253-52-1

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. name: Phthalazine

Heterocyclic Nanographenes and Other Polycyclic Heteroaromatic Compounds: Synthetic Routes, Properties, and Applications

Two-dimensionally extended, polycyclic heteroaromatic molecules (heterocyclic nanographenes) are a highly versatile class of organic materials, applicable as functional chromophores and organic semiconductors. In this Review, we discuss the rich chemistry of large heteroaromatics, focusing on their synthesis, electronic properties, and applications in materials science. This Review summarizes the historical development and current state of the art in this rapidly expanding field of research, which has become one of the key exploration areas of modern heterocyclic chemistry.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N419 – PubChem

Chemistry is traditionally divided into organic and inorganic chemistry. Recommanded Product: 253-52-1, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 253-52-1

Phthalazine-triones: Calix[4]arene-assisted synthesis using green solvents and their anticancer activities against human cancer cells

Fourteen phthalazine-triones bearing different substituents at C-4 position were synthesized through multicomponent reactions (MCR) by using phthalhydrazide, dimedone and diferent aldehydes as starting materials, p-sulfonic acid calix[4]arene as catalyst and ethyl lactate as solvent under microwave irradiation. Compounds 7?16 were obtained in excellent to moderate yields (94?51%) in only 10 min of reaction using this methodology. The antiproliferative activity against cancer cells was disclosed, for the first time, for synthesized compounds. The capacity of all compounds to inhibit cancer cells growth was dependent on the histological origin of cells. Compound 20 was active against more than one strain.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N361 – PubChem

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L-4, a well-tolerated and orally active inhibitor of hedgehog pathway, exhibited potent anti-tumor effects against medulloblastoma in vitro and in vivo

Inhibition of aberrant Hedgehog (Hh) pathway had been proved to be a promising therapeutic intervention in cancers like basal cell carcinoma (BCC), medulloblastoma (MB), and so on. Two drugs (Vismodegib, Sonidegib) were approved to treat BCC and more inhibitors are in clinical investigation. However, the adverse effects and drug resistance restricted the use of Hh inhibitors. In the present study, 61 synthesized compounds containing central backbone of phthalazine or dimethylpyridazine were screened as candidates of new Hh signaling inhibitors by performing dual luciferase reporter assay. Among the compounds, L-4 exhibited an IC50 value of 2.33 nM in the Shh-Light II assay. L-4 strongly inhibited the Hh pathway in vitro and blocked the Hh pathway by antagonizing the smoothened receptor (Smo). Remarkably, L-4 could significantly suppress the Hh pathway activity provoked by Smo mutant (D473H) which showed strong resistant properties to existing drugs such as Vismodegib. Orally administered L-4 exhibited prominent dose-dependent anti-tumor efficacy in vivo in Ptch+/-; p53-/- MB allograft model. Furthermore, L-4 showed good tolerance in acute toxicity test using ICR mice. These evidences indicated that L-4 was a potent, well-tolerated, orally active inhibitor of Hedgehog pathway, and might be a promising candidate in development of Hh-targeted anti-cancer drugs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N515 – PubChem

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1,3-Dipolar Cycloaddition of Ylides Generated from Diazines and Dichlorocarbene

Reaction of dichlorocarbene with diazines in the presence of dimethyl maleate and dimethyl acetylenedicaroxylate involves intermediate formation of ylides, namely cycloimmoniodichloromethanides, followed by 1,3-dipolar cycloaddition of the latter to dipolarophiles. This carbene-ylide sequence was used to synthesize chloro-substituted pyrrolo[1,2-6]pyridazines, pyrrolo[1,2-c]- and pyrrolo[1,2-a]pyrimidines, pyrrolo[1,2-a]phthalazine, pyrrolo[1,2-a]-, pyrrolo[1,2-c]-, and pyrrolo[2,1-b]quinazolines, pyrrolo[1,2-a]-quinoxalines, and pyrrolo[1,2-a]naphthiridines. The cycloaddition is stereo- and regioselective, which suggests a concerted reaction mechanism. The regioselectivity of the cycloaddition is correctly predicted in terms of the PMO theory on the basis of MNDO electronic parameters of halogenated cycloimmonium ylides.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N234 – PubChem

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Insertion of Isocyanides into N?Si Bonds: Multicomponent Reactions with Azines Leading to Potent Antiparasitic Compounds

Trimethylsilyl chloride is an efficient activating agent for azines in isocyanide-based reactions, which then proceed through a key insertion of the isocyanide into a N?Si bond. The reaction is initiated by N activation of the azine, followed by nucleophilic attack of an isocyanide in a Reissert-type process. Finally, a second equivalent of the same or a different isocyanide inserts into the N?Si bond leading to the final adduct. The use of distinct nucleophiles leads to a variety of alpha-substituted dihydroazines after a selective cascade process. Based on computational studies, a mechanistic hypothesis for the course of these reactions was proposed. The resulting products exhibit significant activity against Trypanosoma brucei and T. cruzi, featuring favorable drug-like properties and safety profiles.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N238 – PubChem

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Alcohols as alkylating agents in heteroarene C-H functionalization

Redox processes and radical intermediates are found in many biochemical processes, including deoxyribonucleotide synthesis and oxidative DNA damage. One of the core principles underlying DNA biosynthesis is the radical-mediated elimination of H2O to deoxygenate ribonucleotides, an example of ‘spin-centre shift’, during which an alcohol C-O bond is cleaved, resulting in a carbon-centred radical intermediate. Although spin-centre shift is a well-understood biochemical process, it is underused by the synthetic organic chemistry community. We wondered whether it would be possible to take advantage of this naturally occurring process to accomplish mild, non-traditional alkylation reactions using alcohols as radical precursors. Because conventional radical-based alkylation methods require the use of stoichiometric oxidants, increased temperatures or peroxides, a mild protocol using simple and abundant alkylating agents would have considerable use in the synthesis of diversely functionalized pharmacophores. Here we describe the development of a dual catalytic alkylation of heteroarenes, using alcohols as mild alkylating reagents. This method represents the first, to our knowledge, broadly applicable use of unactivated alcohols as latent alkylating reagents, achieved via the successful merger of photoredox and hydrogen atom transfer catalysis. The value of this multi-catalytic protocol has been demonstrated through the late-stage functionalization of the medicinal agents, fasudil and milrinone.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N213 – PubChem

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Quinoxaline and quinoxaline-1,4-di-N-oxides: An emerging class of antimycobacterials

Tuberculosis (TB) is a highly dreaded, infectious, chronic, airborne disease affecting more than two million people all around the world, with more than eight million cases every calendar year. TB is the second leading infectious cause of death after HIV/AIDS. Over the past few decades, numerous efforts have been undertaken to develop new anti-TB agents. The current frontline therapy for TB consists of administering three or more different drugs (usually isoniazid, rifampin, pyrazinamide, and ethambutol) over an extended period of time. But these drugs will take 6?12 months to cure TB, along with many side effects; hence, there is an urgent need to explore new anti-TB agents. Quinoxaline derivatives are a class of compounds that show a spectrum of biological properties and the interest in these compounds is exponentially growing within the field of medicinal chemistry. Quinoxaline-1,4-di-N-oxide derivatives have shown to improve the biological results and are endowed with anti-viral, anti-cancer, anti-bacterial, and anti-protozoal activities with application in many other therapeutic areas. Since quinoxaline derivatives are regarded as a new class of effective anti-TB candidates, their 1,4-di-N-oxide analogues may show promising in vitro and in vivo anti-TB activities and might be able to prevent the drug resistance to a certain extent. Therefore, the main aim of this review is to focus on important quinoxaline and quinoxaline-1,4-di-N-oxide analogues that have shown anti-TB activities, and their structure?activity relationships for designing anti-TB agents with better efficacies. The present review will be helpful in providing insights for rational designs of more active and less toxic quinoxaline-based anti-TB prodrugs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N227 – PubChem

Reference of 253-52-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.253-52-1, Name is Phthalazine, molecular formula is C8H6N2. In a Article£¬once mentioned of 253-52-1

Induced Circular Dichroism of beta-Cyclodextrin Complexes with Azanaphthalenes-Polarization Directions of the ?* <- ? Transitions in Azanaphthalenes The induced circular dichroism (ICD) spectra of cyclodextrin (beta-CDx) complexes with mono-, di-, and triazanaphthalenes were measured in the wavelength region 200-400 nm.The polarization analysis and spectral assignements of these azanaphthalenes were made from the comparison of the theoretical results calculated by using the CNDO/C-SI approximation with the observed ICD spectra.The polarization directions of the first ?* <- ? transition in azanaphthalenes are closely related to the position of aza nitrogen and can be determined by the coefficients of the configurations in corresponding lowest ?* <- ? states.From the observation of the ICD bands with mixed signs, the presence of the "forbidden" character is strongly suggested in the second absorption bands of isoquinoline, cinnoline, and quinazoline.In each case of azanaphthalenes, the observation of positive ICD bands in the third absorption band indicated the predominance of the long-axis-polarized electronic transition. 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.Reference of 253-52-1

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Phthalazine – Wikipedia,
Phthalazine | C8H6N407 – PubChem

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. HPLC of Formula: C8H6N2

Visible-Light-Initiated Manganese Catalysis for C?H Alkylation of Heteroarenes: Applications and Mechanistic Studies

A visible-light-driven Minisci protocol that employs an inexpensive earth-abundant metal catalyst, decacarbonyldimanganese Mn2(CO)10, to generate alkyl radicals from alkyl iodides has been developed. This Minisci protocol is compatible with a wide array of sensitive functional groups, including oxetanes, sugar moieties, azetidines, tert-butyl carbamates (Boc-group), cyclobutanes, and spirocycles. The robustness of this protocol is demonstrated on the late-stage functionalization of complex nitrogen-containing drugs. Photophysical and DFT studies indicate a light-initiated chain reaction mechanism propagated by .Mn(CO)5. The rate-limiting step is the iodine abstraction from an alkyl iodide by .Mn(CO)5.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N322 – PubChem

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A simple and efficient method for the preparation of N- heteroaromatic N-oxides

Urea-hydrogen peroxide/formic acid system has shown utility for mild and safe N-oxidation of N-heteroaromatic compounds.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N52 – PubChem