Category: pyridazine

COA of Formula: C10H9NO2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Modulation of the antitumor activity by methyl substitutions in the series of 7H-pyridocarbazole monomers and dimers. Author is Leon, P.; Garbay-Jaureguiberry, C.; Barsi, M. C.; Le Pecq, J. B.; Roques, Bernard P..

The structure of the dimeric antitumor drug ditercalinium (NSC 366241) [2,2′-([4,4′-bipiperidine]-1,1′-diyldi-2,1-ethanediyl)bis[10-methoxy-7H-pyrido[4,3-c]carbazolium] tetramethanesulfonate] was modified by introduction of Me groups in various positions of the aromatic ring. Methylation of 7H-pyridocarbazoles on position 7 was performed by reaction with NaH followed by MeI addition methylation at the 5- or 6-position required a total synthesis of the pyridocarbazole ring, including photocyclization of the appropriately substituted indolylpyridylethylene. Thus, 7H-pyridocarbazole monomers, e.g., 5-Me derivative I, and dimers, e.g. 6-Me derivative II, were prepared Monomeric analogs with the nitrogen atom of the pyridine ring in different positions have also been synthesized. Pharmacol. properties and DNA interactions of the new compounds are reported. In contrast with the monomeric analog of ditercalinium, which was inactive, Me substitutions on the 10-methoxy-7H-pyrido[4,3-c]carbazolium in positions 6 or 7 led to monomers endowed with small but significant activity. Dimerization of the methyl-substituted pyridocarbazoles yielded DNA bisintercalators with affinity slightly higher than that of the unsubstituted parent compounds These dimers, characterized by a relatively better therapeutic index, have the same mechanism of action as ditercalinium. Otherwise, in monomeric and dimeric series, Me substitution in position 4 or 5 provided inactive compounds unable to intercalate into DNA. All these results are in agreement with the previously proposed geometry for the complex of ditercalinium with DNA.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about N-heterocyclic carbene catalyzed domino reactions of formylcyclopropane 1,1-diesters: construction of a 6-5-5 tricyclic pyrrolo[1,2-a]indole.Quality Control of 5-Methoxy-1H-indole-2-carbaldehyde.

Catalyzed by N-heterocyclic carbenes (NHCs), a domino ring-opening/redox amidation/Knoevenagel condensation of readily available formylcyclopropane 1,1-diesters with 1H-indole-2-carbaldehydes is reported. This methodol. provides a new and direct method for the construction of a 6-5-5 tricyclic pyrrolo[1,2-a]indole skeleton I (R1 = H, 5-Me, 5-MeO, 5-Et, 5-iPr, 5-Cl, R2 = CO2Et, R3 = Et, R4 = H; R1 = R4 = H, R2 = CO2Me, R3 = Me; R1 = R4 = H,R2 = CO2iPr, R3 = Et; R1 = H, R2 = CO2Et, R3 = Et, R4 = Me; R1 = H, 5-Me, 5-Cl, R2 = H, R3 = Et, R4 = H).

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Computed Properties of C7H13BrO2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Gold-catalysed asymmetric net addition of unactivated propargylic C-H bonds to tethered aldehydes. Author is Li, Ting; Cheng, Xinpeng; Qian, Pengcheng; Zhang, Liming.

The asym. one-step net addition of unactivated propargylic C-H bonds to aldehydes such as 7-(dimethyl(phenyl)silyl)hept-6-ynal, 4-(benzyloxy)-7-(tert-butyldimethylsilyl)hept-6-ynal, 7-(tert-Butyldimethylsilyl)-2-phenylhept-6-ynal, etc. leads to an atom-economic construction of versatile chiral homopropargylic alcs. e.g., I, but has not yet been realized. Here, implementation in an intramol. manner under mild reaction conditions have been showed. This chem.-via cooperative gold catalysis enabled by chiral bifunctional phosphine ligands (1R/1S)-II (R = Me, Cy; R1 = H, Me)-achieves asym. catalytic deprotonation of propargylic C-H (pKa > 30) by a tertiary amine group (pKa ≈ 10) of the ligand in the presence of much more acidic aldehydic α-hydrogens (pKa ≈ 17). The reaction exhibits a broad scope and readily accommodates various functional groups. The cyclopentane/cyclohexane-fused homopropargylic alc. products e.g., III are formed with excellent enantiomeric excesses and high trans-selectivities with or without a preexisting substrate chiral center. D. functional theory studies of the reaction support the conceived reaction mechanism and the calculated energetics corroborate the observed stereoselectivity and confirm addnl. metal-ligand cooperation.

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The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 5-Methoxy-1H-indole-2-carbaldehyde(SMILESS: O=CC(N1)=CC2=C1C=CC(OC)=C2,cas:21778-81-4) is researched.Computed Properties of C7H13BrO2. The article 《Copper-Catalyzed Annulation of 2-Formylazoles with o-Aminoiodoarenes》 in relation to this compound, is published in Journal of Organic Chemistry. Let’s take a look at the latest research on this compound (cas:21778-81-4).

In the presence of catalytic CuI and sparteine, 2-formylpyrroles can be annulated with o-aminoiodoarenes to give substituted pyrrolo[1,2-a]quinoxalines and related heterocycles. The reaction also works for annulation of 2-formylindoles, 2-formylimidazole, 2-formylbenzimidazole, and a 3-formylpyrazole.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Organic & Biomolecular Chemistry called Pd-catalyzed cascade allylic alkylation and dearomatization reactions of indoles with vinyloxirane, Author is Gao, Run-Duo; Xu, Qing-Long; Dai, Li-Xin; You, Shu-Li, which mentions a compound: 21778-81-4, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2, Electric Literature of C10H9NO2.

A palladium-catalyzed cascade allylic alkylation reaction of di-Me malonate tethered indoles with vinyloxirane was developed through intramol. nucleophilic ring-opening of vinyloxirane followed by subsequent intramol. Friedel-Crafts type allylic alkylation or allylic dearomatization. This protocol provided an efficient method to synthesize structurally diverse tetrahydrocarbolines e.g., I, and spiroindolenine derivatives e.g., II, under mild conditions.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ) is researched.Category: pyridazine.Das, Tapas; Kayet, Anirban; Mishra, Ruchika; Singh, Vinod K. published the article 《Highly fluorescent 1,2-dihydropyrimido[1,6-α]indoles: an efficient metal-free synthesis and photophysical study》 about this compound( cas:21778-81-4 ) in Chemical Communications (Cambridge, United Kingdom). Keywords: dihydropyrimidoindole preparation; indole carboxaldehyde ethyl arylideneglycinate aldol Mannich reaction. Let’s learn more about this compound (cas:21778-81-4).

A metal-free route to highly fluorescent 1,2-dihydropyrimido[1,6-α]indole derivatives I (R = H, OCH3, CH3, Br; Ar = C6H5, naphth-1-yl, furan-2-yl, etc.) has been developed via base catalyzed aldol followed by the Mannich reaction of indole-2-carboxaldehydes II with Et N-arylideneglycinates ArHC=NCH2COOEt at room temperature This transformation consists of the sequential formation of two new bonds to afford highly functionalized pyrimidoindole derivatives under mild reaction conditions.. Photophys. properties of the products have also been reported.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors》. Authors are Henderson, Scott H.; Sorrell, Fiona; Bennett, James; Fedorov, Oleg; Hanley, Marcus T.; Godoi, Paulo H.; Ruela de Sousa, Roberta; Robinson, Sean; Ashall-Kelly, Alexander; Hopkins Navratilova, Iva; Walter, Daryl S.; Elkins, Jonathan M.; Ward, Simon E..The article about the compound:(R)-(-)-3-Fluoropyrrolidine Hydrochloridecas:136725-55-8,SMILESS:Cl.F[C@@H]1CCNC1).HPLC of Formula: 136725-55-8. Through the article, more information about this compound (cas:136725-55-8) is conveyed.

Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer′s disease (AD) and Down′s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A′s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Synthetic Route of C7H13BrO2. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about New GSH-responsive amphiphilic zinc(II) phthalocyanine micelles as efficient drug carriers for combinatorial cancer therapy. Author is Guo, Shanlei; Gao, Bo; Li, Dongni.

Combination therapies for the treatment of cancer have attracted wide attention. The poor selectivity and biocompatibility of photosensitizers (PS) limit the use of combination therapies in chemotherapy and photodynamic therapy (PDT) for cancer. In this work, the Gender PS (mPEG-b-PLA-S-S-ZnPC), asym. zinc(II) phthalocyanine (ZnPC) and mono-methoxy oxygen-based polyethylene glycol-polylactic acid (mPEG-b-PLA) were designed and synthesized for PDT through disulfide bond (-S-S-). The amphipathic PS could be self-assembled into a micelle in aqueous solution, and paclitaxel (PTX) was encapsulated in the core of the micelle for chemotherapy (PTX/mPEG-b-PLA-S-S-ZnPc). The PTX/mPEG-b-PLA-S-S-ZnPc micelle was spherical with a uniform diameter of about 184 nm. At the first 48 h, the release behaviors of ZnPC and PTX at 10 mmol / L GSH were 30% and 75.2%, resp. These results suggested that GSH-responsive PTX/mPEG-b-PLA-S-S-ZnPc micelle was an active ingredient in combination therapies for cancer.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, RSC Advances called Rhodium(II)-catalyzed intramolecular annulation of 1-sulfonyl-1,2,3-triazoles with indoles: facile synthesis of functionalized tetrahydro-β-carbolines, Author is Shang, Hai; Tian, Yu; Luo, Jun; Li, Lingyu; Tang, Yefeng; Zou, Zhongmei, which mentions a compound: 21778-81-4, SMILESS is O=CC(N1)=CC2=C1C=CC(OC)=C2, Molecular C10H9NO2, Electric Literature of C10H9NO2.

A novel rhodium(II)-catalyzed intramol. annulation of 1-sulfonyl-1,2,3-triazoles with indoles was developed, which enabled the facile synthesis of various 4-functionalized tetrahydro-β-carbolines as well as relevant scaffolds from readily available starting materials.

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Recommanded Product: 21778-81-4. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Amide-Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility. Author is Tan, Yu Jia; Li, Ming; Gunawan, Gregory Adrian; Nyantakyi, Samuel Agyei; Dick, Thomas; Go, Mei-Lin; Lam, Yulin.

Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here, it was found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility Potent activity could be achieved without the carboxamide linker but not in the absence of the indole ring. The indolylmethylamine, N-cyclooctyl-6-trifluoromethylindol-2-ylmethylamine (MIC90Mtb 0.13μM, MBC99.9Mtb 0.63μM), exemplifies a promising member that is more soluble and equipotent to its carboxamide equivalent It is also an inhibitor of the mycolate transporter MmpL3, a property shared by the methylamines of benzothiophene and benzoselenophene.

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Pyridazine – Wikipedia,
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