Month: April 2022

Application of 17739-45-6. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about Sphingomonas montanisoli sp. nov., isolated from mountain soil. Author is Xu, Zixiao; Zhang, Yuxiao; Muhammad, Yasir; Wang, Gejiao.

A soil bacterium, designated ZX9611T, was isolated from Taihang Mountain in Henan province, PR China. The strain was Gram-stain-neg. and strictly aerobic. The cells were motile, rod-shaped and formed light pink-colored colonies. The 16S rRNA gene sequence of ZX9611T shared the highest similarities with those of Sphingomonas crocodyli CCP-7T (97.0%), Sphingomonas jatrophae S5-249T (96.6%) and Sphingomonas starnbergensis 382T (95.9%). Phylogenetic analyses based on 16S rRNA gene sequences demonstrated that ZX9611T clustered with S. crocodyli CCP-7T, S. jatrophae S5-249T and S. starnbergensis 382T. The average nucleotide identity (ANI) values between ZX9611T and two type strains (S. crocodyli BCRC 81096T and S. jatrophae DSM 27345T) were 88.3 and 68.6% resp. ZX9611T exhibited genome-sequence-based digital DNA-DNA hybridization (dDDH) values of 53.3% and 15.3%, compared with S. crocodyli BCRC 81096T and S. jatrophae DSM 27345T, resp. ZX9611T had a genome size of 4.12 Mb and an average DNA G + C content of 64.8%. ZX9611T had major fatty acids (>5%) including summed feature 8 (C18 : 1 ω7c and/or C18 : 1 ω6c), C14 : 0 2-OH, C16 : 0 and summed feature 3 (C16 : 1 ω7c and/or C16 : 1 ω6c), and the major polyamine was sym-homospermidine. The only respiratory quinone was ubiquinone-10. The polar lipids were diphosphatidylglycerol, phosphatidylethanolamine, phosphatidylglycerol, phosphatidylcholine and sphingoglycolipid. On the basis of phenotypic, chemotaxonomic and phylogenetic characteristics, strain ZX9611T represents a novel species of genus Sphingomonas, for which the name Sphingomonas montanisoli sp. nov. is proposed. The type strain is ZX9611T (= KCTC 72622T = CCTCC AB 2019350T).

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Safety of 5-Methoxy-1H-indole-2-carbaldehyde. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthesis and Biological Evaluation of Indolyl-Pyridinyl-Propenones Having Either Methuosis or Microtubule Disruption Activity. Author is Trabbic, Christopher J.; Overmeyer, Jean H.; Alexander, Evan M.; Crissman, Emily J.; Kvale, Heather M.; Smith, Marcie A.; Erhardt, Paul W.; Maltese, William A..

Methuosis is a form of nonapoptotic cell death characterized by an accumulation of macropinosome-derived vacuoles with eventual loss of membrane integrity. Small mols. inducing methuosis could offer significant advantages compared to more traditional anticancer drug therapies that typically rely on apoptosis. Herein we further define the effects of chem. substitutions at the 2- and 5-indolyl positions on our lead compound I. We have identified a number of compounds that induce methuosis at similar potencies, including an interesting analog having a hydroxypropyl substituent at the 2-position. In addition, we have discovered that certain substitutions on the 2-indolyl position redirect the mode of cytotoxicity from methuosis to microtubule disruption. This switch in activity is associated with an increase in potency as large as 2 orders of magnitude. These compounds appear to represent a new class of potent microtubule-active anticancer agents.

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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 Asymmetric construction of polycyclic indole derivatives with different ring connectivities by an organocatalysis triggered two-step sequence.COA of Formula: C10H9NO2.

An organocatalysis triggered highly regio- and stereoselective two-step sequence between hemiacetals and indole-containing nitroolefins was developed. The key to the success of this sequence was the intramol. oxocarbenium ion induced collective alkylation at the C3, C2, or N1-position of the indole moiety, resp., providing biol. important polycyclic indole derivatives with different ring connectivities. An unexpected epimerization was observed during the C3-alkylation process, which generated products with different relative configurations compared with the C2- and N1-alkylation products.

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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: 2-(2-Bromoethoxy)tetrahydro-2H-pyran, is researched, Molecular C7H13BrO2, CAS is 17739-45-6, about VIPP2 interacts with VIPP1 and HSP22E/F at chloroplast membranes and modulates a retrograde signal for HSP22E/F gene expression.SDS of cas: 17739-45-6.

VIPP proteins aid thylakoid biogenesis and membrane maintenance in cyanobacteria, algae, and plants. Some members of the Chlorophyceae contain two VIPP paralogs termed VIPP1 and VIPP2, which originate from an early gene duplication event during the evolution of green algae. VIPP2 is barely expressed under nonstress conditions but accumulates in cells exposed to high light intensities or H2O2, during recovery from heat stress, and in mutants with defective integration (alb3.1) or translocation (secA) of thylakoid membrane proteins. Recombinant VIPP2 forms rod-like structures in vitro and shows a strong affinity for phosphatidylinositol phosphate. Under stress conditions, >70% of VIPP2 is present in membrane fractions and localizes to chloroplast membranes. A vipp2 knock-out mutant displays no growth phenotypes and no defects in the biogenesis or repair of photosystem II. However, after exposure to high light intensities, the vipp2 mutant accumulates less HSP22E/F and more LHCSR3 protein and transcript. This suggests that VIPP2 modulates a retrograde signal for the expression of nuclear genes HSP22E/F and LHCSR3. Immunoprecipitation of VIPP2 from solubilized cells and membrane-enriched fractions revealed major interactions with VIPP1 and minor interactions with HSP22E/F. Our data support a distinct role of VIPP2 in sensing and coping with chloroplast membrane stress.

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Pyridazine – Wikipedia,
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Electric Literature of C4H9ClFN. 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: (R)-(-)-3-Fluoropyrrolidine Hydrochloride, is researched, Molecular C4H9ClFN, CAS is 136725-55-8, about Discovery of novel 4-phenyl-2-(pyrrolidinyl)nicotinamide derivatives as potent Nav1.1 activators. Author is Miyazaki, Tohru; Kawasaki, Masanori; Suzuki, Atsushi; Ito, Yuki; Imanishi, Akio; Maru, Takamitsu; Kawamoto, Tomohiro; Koike, Tatsuki.

The voltage-gated sodium channel, Nav1.1, is predominantly expressed in parvalbumin-pos. fast spiking interneurons and has been genetically linked to Dravet syndrome. Starting from a high throughput screening hit isoxazole derivative 5, modifications of 5 via combinations of IonWorks and Q-patch assays successfully identified the nicotinamide derivative 4. Its increasing decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 and acceptable brain exposure in mice was observed Compound 4 is a promising Nav1.1 activator that can be used to analyze pathophysiol. functions of the Nav1.1 channel towards treating various central nervous system diseases.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

COA of Formula: C10H9NO2. 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: 5-Methoxy-1H-indole-2-carbaldehyde, is researched, Molecular C10H9NO2, CAS is 21778-81-4, about Synthesis of 9H-Pyrrolo[1,2-a]indole and 3H-Pyrrolizine Derivatives via a Phosphine-Catalyzed Umpolung Addition/Intramolecular Wittig Reaction. Author is Saleh, Nidal; Voituriez, Arnaud.

The first umpolung addition/intramol. Wittig reaction, catalytic in phosphine, is described. The in situ phosphine oxide reduction was accomplished by the use of silane and a catalytic amount of bis(4-nitrophenyl)phosphate. This catalytic protocol is applicable to the synthesis of a wide range of functionalized 9H-pyrrolo[1,2-a]indoles and pyrrolizines (18 examples, 70-98% yields).

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Pyridazine – Wikipedia,
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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.Safety of 5-Methoxy-1H-indole-2-carbaldehyde.Kuwano, Satoru; Suzuki, Takumi; Yamanaka, Masahiro; Tsutsumi, Ryosuke; Arai, Takayoshi published the article 《Catalysis based on C-I···π halogen bonds: electrophilic activation of 2-alkenylindoles by cationic halogen-bond donors for [4+2] cycloadditions》 about this compound( cas:21778-81-4 ) in Angewandte Chemie, International Edition. Keywords: alkenylindole iodoimidazolium triflate catalyst diastereoselective cycloaddition; indolyl tetrahydrocarbazole preparation; cycloaddition; density-functional calculations; halogen bonding; heterocycles; noncovalent bonds. Let’s learn more about this compound (cas:21778-81-4).

Homo- and cross-[4+2] cycloadditions of 2-alkenylindoles catalyzed by cationic halogen-bond donors were developed. Under mild reaction conditions, 3-indolyl-substituted tetrahydrocarbazole derivatives were obtained in good to excellent yields. Exptl. and quantum calculation studies revealed that the electrophilic activation of 2-alkenylindoles was achieved by C-I···π halogen bonds.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Dawange, Monali A.; Urmode, Tukaram D.; Khan, Ayesha; Kusurkar, Radhika S. published the article 《Acid Catalyzed Synthesis of Spiroindolone Scaffolds by Iso-Pictet-Spengler Spirocyclization and Evaluation of their Antibacterial Activity》. Keywords: spiroindolone preparation antibacterial; isatin isotryptamine iso Pictet Spengler spirocyclization acetic acid catalyst.They researched the compound: 5-Methoxy-1H-indole-2-carbaldehyde( cas:21778-81-4 ).HPLC of Formula: 21778-81-4. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:21778-81-4) here.

Acetic acid catalyzed synthesis of new spiroindolones (tetrahydrospiro-γ-carbolines) was achieved in good yield by iso-Pictet Spengler spirocyclization of substituted isotryptamines with isatins. All the compounds were screened for antibacterial activities against S. aureus, E. coli, P. aeruginosa and S. typhi bacteria. The preliminary antibacterial study indicated that compounds bearing halo substituent showed potent inhibitory activity towards S. typhi and P. aeruginosa and moderate activities towards S. aureus and E. coli.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Scalable Process Design for a PDE10A Inhibitor Consisting of Pyrazolopyrimidine and Quinoxaline as Key Units, published in 2019-04-19, which mentions a compound: 136725-55-8, Name is (R)-(-)-3-Fluoropyrrolidine Hydrochloride, Molecular C4H9ClFN, Reference of (R)-(-)-3-Fluoropyrrolidine Hydrochloride.

In this study, research and development for the synthetic process of a PDE10A inhibitor are described; in particular, an efficient regioselective construction of the quinoxaline unit, a cost-effective pyrazolo[1,5-a]pyrimidine formation, and a cost-saving approach in a nucleophilic aromatic substitution (SNAr) reaction by introducing oxazolidinone as an electron-withdrawing group to a chloropyrazolo[1,5-a]pyrimidine core are key points. The newly developed process has been successfully scaled up to 40 kg. Furthermore, a one-pot tandem reaction from aminopyrazole to dichloropyrazolo[1,5-a]pyrimidine by activating malonic acid with POCl3 was discovered. The finding contributed to avoiding isolation of the hygroscopic pyrazolo[1,5-a]pyrimidin-5(4H)-one intermediate, which caused complicated filtration and drying processes observed in the first scale-up campaign.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Lindsay-Scott, Peter J.; Rivlin-Derrick, Eloise researched the compound: 2-(2-Bromoethoxy)tetrahydro-2H-pyran( cas:17739-45-6 ).Quality Control of 2-(2-Bromoethoxy)tetrahydro-2H-pyran.They published the article 《Regiocontrolled Synthesis of 6,7-Dihydro-4H-pyrazolo[5,1-c][1,4]oxazines》 about this compound( cas:17739-45-6 ) in Synthesis. Keywords: dihydropyrazolooxazine regioselective preparation. We’ll tell you more about this compound (cas:17739-45-6).

Synthesis of 6,7-dihydro-4H-pyrazolo[5,1- c][1,4]oxazines wad achieved in 3-4 steps from com. available pyrazoles. Optimization of a protected hydroxyethyl group on N1 enabled the regiocontrolled construction of pyrazole-5-aldehydes in high yields; subsequent deprotection and reduction generated fused heterocyclic scaffolds bearing multiple substitution patterns. Moreover, the intermediate pyrazole lactols were showed to be versatile synthetic building blocks.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem