Month: October 2022

Bennasar, M.-Lluiesa; Zulaica, Ester; Juan, Cecilia; Alonso, Yolanda; Bosch, Joan published the artcile< Addition of Ester Enolates to N-Alkyl-2-fluoropyridinium Salts: Total Synthesis of (±)-20-Deoxycamptothecin and (+)-Camptothecin>, Related Products of 131747-55-2, the main research area is ester enolate addition fluoropyridinium salt; deoxycamptothecin total synthesis; camptothecin total synthesis.

Several 4-substituted dihydropyridones or 2-pyridones have been prepared by nucleophilic addition of α-(methylsulfanyl)ester enolates to N-alkyl-2-fluoropyridinium salts, followed by acid hydrolysis or oxidation with concomitant hydrolysis, of the intermediate 2-fluoro-1,4-dihydropyridine adducts, resp. Addition of the enolate derived from iso-Pr α-(methylsulfanyl)butyrate to N-(quinolylmethyl)-2-fluoropyridinium triflate followed by DDQ treatment gave a pyridone I, from which (±)-20-deoxycamptothecin a known precursor of camptothecin was synthesized by a radical cyclization-desulfurization, with subsequent elaboration of the lactone E ring by chemoselective reduction A similar sequence starting from the enolate of a chiral 2-hydroxybutyric acid derivative (II) provides access to natural (+)-camptothecin.

Journal of Organic Chemistry published new progress about Addition reaction. 131747-55-2 belongs to class pyridine-derivatives, and the molecular formula is C6H6FNO, Related Products of 131747-55-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Ruixin; Wang, Liang; Zhang, Kena; Li, Jingya; Zou, Dapeng; Wu, Yangjie; Wu, Yusheng published the artcile< Facile synthesis of trifluoroethyl aryl ethers through copper-catalyzed coupling of CF3CH2OH with aryl- and heteroaryl boronic acids>, Related Products of 832735-54-3, the main research area is trifluoroethyl aryl ether preparation catalytic Chan Lam coupling reaction; trifluoroethanol coupling aryl boronic acid copper catalyst.

An efficient copper-catalyzed Chan-Lam reaction of trifluoroethanol with a variety of aryl- and heteroaryl boronic acids has been developed. This research provides a practical method to synthesize trifluoroethyl aryl ethers in moderate to good yields under mild conditions.

Tetrahedron Letters published new progress about Alkyl aryl ethers Role: SPN (Synthetic Preparation), PREP (Preparation). 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, Related Products of 832735-54-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jalba, Angela; Levitre, Guillaume; Keipour, Hoda; Lauzon, Samuel; Ollevier, Thierry published the artcile< New chiral bis(oxazolinyl)bipyridine ligands and application in the iron catalyzed asymmetric hydrosilylation of ketones>, Electric Literature of 147409-41-4, the main research area is chiral bis oxazolinyl bipyridine ligand preparation catalyst; iron catalyzed asym hydrosilylation acetophenone ketone.

C2 sym. 6,6′-bis(oxazolinyl)-2,2′-bipyridine (bipybox) chiral ligands have been synthesized from readily available 2,2′-bipyridine. Catalytic asym. hydrosilylation of ketones was studied using this family of ligands in the presence of iron(II) acetate.

French-Ukrainian Journal of Chemistry published new progress about Chiral ligands Role: CAT (Catalyst Use), RCT (Reactant), SPN (Synthetic Preparation), USES (Uses), RACT (Reactant or Reagent), PREP (Preparation). 147409-41-4 belongs to class pyridine-derivatives, and the molecular formula is C22H26N4O2, Electric Literature of 147409-41-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Guo, Xuan; Lv, Fang; Zhao, Zifeng; Gu, Jiannan; Qu, Bo; Xiao, Lixin; Chen, Zhijian published the artcile< Spirobifluorene-based oligopyridine derivatives as electron-transporting materials for green phosphorescent organic light-emitting diodes>, Synthetic Route of 329214-79-1, the main research area is spirobifluorene oligopyridine electron transporting material phosphorescent OLED.

The electron-transporting materials (ETMs), 2,7-bis(3,5-di (pyridin-3-yl)phenyl)-9,9′-spirobi [fluorene] (3-4PySF) and 2,7-bis(3,5-di (pyridin-4-yl)phenyl)-9,9′-spirobi [fluorene] (4-4PySF) were designed and synthesized by combining spirobifluorene moiety with di(pyridine-3-yl)phenyl and di(pyridine-4-yl)phenyl, resp. The spirobifluorene moiety improves materials’ rigid twisted structure to ensure the morphol. stability of amorphous film, and pyridine acts as electron acceptor to enhance electron-transporting ability of materials. The dependence of electron-transporting property on the position of substituted pyridine rings was studied. The m.p. (Tm) of 4-4PySF is estimated to be 41°C higher than that of 3-4PySF. And the higher c.d. in the electron only devices exhibited by 4-4PySF revealed the effect of nitrogen atom position on the charge-transporting properties. Green PhOLEDs based on bis(2-phenylpyridine)iridium (III) (2,2,6,6-tetramethylheptane-3,5-diketonate) (Ir (ppy)2tmd) as the emitter and 3-4PySF, 4-4PySF and 1,3,5-tris(N-phenylbenzimid azol-2-yl-benzene (TPBi) as ETMs were fabricated. Compared to the device based on the conventional ETM TPBi, the devices based on new ETMs exhibited a higher maximum external quantum efficiency (EQE) of 20.5% and a lower turn-on voltage (Von) of 2.6 V.

Organic Electronics published new progress about Crystal structure. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Synthetic Route of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Patel, P. N.; Desai, D. H.; Patel, N. C. published the artcile< Novel Terpyridine Derivatives of Benzothiazole and Copper(II) Complex: Synthesis and Spectral Studies>, Application In Synthesis of 350-03-8, the main research area is crystal structure copper benzothiazolylterpyridine complex; benzothiazolylterpyridine preparation copper complex.

Novel terpyridine derivatives of benzothiazole were synthesized by simple multicomponent 1-pot reaction of benzothiazole-2-carbaldehyde, ammonium hydroxide, and isomeric acetyl pyridines with isolated yields of 92-98%. All the prepared derivatives were characterized by NMR, IR, and high-resolution mass spectra. A Cu(II) complex was prepared selectively from the terpyridine derivative obtained from 2-acetylpyridine and was characterized by single-crystal x-ray anal. UV-visible spectra were recorded for all the synthesized compounds

Russian Journal of Organic Chemistry published new progress about Crystal structure. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Application In Synthesis of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Goldberg, Frederick W.; Finlay, M. Raymond V.; Ting, Attilla K. T.; Beattie, David; Lamont, Gillian M.; Fallan, Charlene; Wrigley, Gail L.; Schimpl, Marianne; Howard, Martin R.; Williamson, Beth; Vazquez-Chantada, Mercedes; Barratt, Derek G.; Davies, Barry R.; Cadogan, Elaine B.; Ramos-Montoya, Antonio; Dean, Emma published the artcile< The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-7,9-dihydro-8H-purin-8-one (AZD7648), a Potent and Selective DNA-Dependent Protein Kinase (DNA-PK) Inhibitor>, Recommanded Product: 6-Amino-3-nitro-2-picoline, the main research area is AZD7648 preparation DNA protein kinase inhibitor cancer.

DNA-PK is a key component within the DNA damage response, as it is responsible for recognizing and repairing double-strand DNA breaks (DSBs) via non-homologous end joining. Historically it has been challenging to identify inhibitors of the DNA-PK catalytic subunit (DNA-PKcs) with good selectivity vs. the structurally related PI3 (lipid) and PI3K-related protein kinases. We screened our corporate collection for DNA-PKcs inhibitors with good PI3 kinase selectivity, identifying compound 1. Optimization focused on further improving selectivity while improving phys. and pharmacokinetic properties, notably co-optimization of permeability and metabolic stability, to identify compound 16 (AZD7648). Compound 16 had no significant off-target activity in the protein kinome and only weak activity vs. PI3Kα/γ lipid kinases. Monotherapy activity in murine xenograft models was observed, and regressions were observed when combined with inducers of DSBs (doxorubicin or irradiation) or PARP inhibition (olaparib). These data support progression into clin. studies (NCT03907969).

Journal of Medicinal Chemistry published new progress about Antitumor agents (potential as). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Recommanded Product: 6-Amino-3-nitro-2-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kucharska, E.; Hanuza, J.; Lorenc, J. published the artcile< Conformation of azo-bridge in 3,3'-dinitro-2,2'-azobipyridine and its 4,4'(or 5,5' or 6,6')-dimethyl-derivatives: Vibrational studies and DFT quantum chemical calculations>, Product Details of C6H5FN2O2, the main research area is conformation azo bridge dinitroazobipyridine dimethylderivative vibrational DFT quantum; Azopyridines; IR and Raman spectra; Methyl and nitro groups; Quantum chemical calculations; Vibrational characteristics of the azo-bond.

Syntheses of 3,3′-dinitro-2,2′-azobipyridine and 4,4′ (or 5,5′ or 6,6′)-dimethyl-3,3′-dinitro-2,2′-azobipyridine were described. Mol. structures of these compounds were determined and compared, to the basic compound, azobipyridine, reported by us earlier. The conformation of the azo-bond and other structural data are discussed in terms of substitution place of Me chromophore. FTIR and Raman spectra of these compounds were measured and analyzed. The 6-311G (2d,2p) basis set with the B3LYP functional were used to discuss the space conformation and dynamics of the studied compounds

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Chromophores. 19346-45-3 belongs to class pyridine-derivatives, and the molecular formula is C6H5FN2O2, Product Details of C6H5FN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Campos, Debora L.; Machado, Ignacio; Ribeiro, Camila M.; Gambino, Dinorah; Pavan, Fernando R. published the artcile< Bactericidal effect of pyridine-2-thiol 1-oxide sodium salt and its complex with iron against resistant clinical isolates of Mycobacterium tuberculosis>, Category: pyridine-derivatives, the main research area is Mycobacterium antibacterial pyridine thiol oxide sodium salt.

We determined the activity of pyridine-2-thiol 1-oxide sodium salt (Na mpo) and its complex with iron [Fe(mpo)3] against Mycobacterium tuberculosis. The compounds were tested against a standard strain of M. tuberculosis H37Rv (ATCC 27294), with minimal inhibitory concentrations (MIC90) of 7.20 and 1.07 μM to Na mpo and [Fe(mpo)3], resp., and against 3 clin. isolates with different genotypic profiles, with MIC values ranging 0.74-6.52 and 0.30-2.25 μM to Na mpo and [Fe(mpo)3], resp. [Fe(mpo)3] was more effective against susceptible strains but both compounds were effective in inhibiting MDR and XDR-TB clin. strains. The profile activity was determined through the methodol. of a time-kill curve against standard and clin. strains of M. tuberculosis. Time-kill studies indicated that Na mpo had an early bactericidal activity against H37Rv and clin. isolates, with sterilizing effects observed in 5 and 7 days, resp., at its MIC90. The anti MDR and XDR-M. tuberculosis activity and bactericidal effect of Na mpo and [Fe(mpo)3] demonstrate their potential as new compounds for the treatment of tuberculosis.

Journal of Antibiotics published new progress about Mycobacterium tuberculosis. 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Garrett, Mark D.; Scott, Robin; Sheldrake, Gary N.; Dalton, Howard; Goode, Paul published the artcile< Biotransformation of substituted pyridines with dioxygenase-containing microorganisms>, Product Details of C5H4ClNO, the main research area is toluene dioxygenase substituted pyridine oxidation.

A series of 2-, 3- and 4-substituted pyridines was metabolized using the mutant soil bacterium Pseudomonas putida UV4 which contains a toluene dioxygenase (TDO) enzyme. The regioselectivity of the biotransformation in each case was determined by the position of the substituent. 4-Alkylpyridines were hydroxylated exclusively on the ring to give the corresponding 4-substituted 3-hydroxypyridines, while 3-alkylpyridines were hydroxylated stereoselectively on C-1 of the alkyl group with no evidence of ring hydroxylation. 2-Alkylpyridines gave both ring and side-chain hydroxylation products. Chloro- and bromo-substituted pyridines, and pyridine itself, while being poor substrates for P. putida UV4, were converted to some extent to the corresponding 3-hydroxypyridines. These unoptimized biotransformations are rare examples of the direct enzyme-catalyzed oxidation of pyridine rings and provide a novel synthetic method for the preparation of substituted pyridinols. Evidence for the involvement of the same TDO enzyme in both ring and side-chain hydroxylation pathways was obtained using a recombinant strain of Escherichia coli (pKST11) containing a cloned gene for TDO. The observed stereoselectivity of the side-chain hydroxylation process in P. putida UV4 was complicated by the action of an alc. dehydrogenase enzyme in the organism which slowly leads to epimerization of the initial (R)-alc. bioproducts by dehydrogenation to the corresponding ketones followed by stereoselective reduction to the (S)-alcs.

Organic & Biomolecular Chemistry published new progress about Oxidation, regioselective. 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Product Details of C5H4ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem