Tag: M.W=150-200

Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L.; Filipski, Kevin J.; He, Mingying; Zhou, Ru; Ahmed, Syed; Benbow, John; Perez, Angel-Guzman; Tu, Meihua; Litchfield, John; Sharma, Raman; Metzler, Karen; Bourbonais, Francis; Huang, Cong; Beebe, David A.; Oates, Peter J. published the artcile< Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle>, Name: 4,5-Dichloropyridin-2-amine, the main research area is aminopicoline carboxylic acid cyclization transamidation; sulfonyl pyridone preparation glucokinase activation antidiabetic human.

A promising area of novel anti-diabetic therapy involves identification of small mol. activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, the identification and optimization of a series of 4-sulfonyl-2-pyridone, i.e. I, activators is reported. The activators were evaluated for in vitro biochem. activation and pharmacokinetic properties. As part of these efforts, a unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymic conditions.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Name: 4,5-Dichloropyridin-2-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wagener, Tobias; Heusler, Arne; Nairoukh, Zackaria; Bergander, Klaus; Daniliuc, Constantin G.; Glorius, Frank published the artcile< Accessing (Multi)Fluorinated Piperidines Using Heterogeneous Hydrogenation>, Category: pyridine-derivatives, the main research area is fluoropiperidine diastereoselective preparation; palladium heterogeneous catalyst stereoselective hydrogenation fluoropyridine.

Fluorinated piperidines are desirable motifs for pharmaceutical and agrochem. research. Nevertheless, general synthetic access remains out of reach. Herein, we describe a simple and robust cis-selective hydrogenation of abundant and cheap fluoropyridines to yield a broad scope of (multi)fluorinated piperidines. This protocol enables the chemoselective reduction of fluoropyridines while tolerating other (hetero)aromatic systems using a com. available heterogeneous catalyst. Fluorinated derivatives of important drug compounds are prepared, and a straightforward strategy for the synthesis of enantioenriched fluorinated piperidines is disclosed.

ACS Catalysis published new progress about Aryl fluorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (fluoropyridines). 876919-08-3 belongs to class pyridine-derivatives, and the molecular formula is C7H6FNO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pegu, David published the artcile< Analysis of molecular structure, vibrational spectra and electronic properties of 2-amino-3-nitro-6-picoline by density functional methods>, Recommanded Product: 2-Amino-3-nitro-6-picoline, the main research area is amino nitro picoline mol structure IR Raman electrostatic potential.

In the present study the geometrical parameters and vibrational spectroscopic properties of the compound 2-amino-3-nitro-6-picoline (2A3N6P) have been calculated by using Harteree-Fock and D. functional method (B3LYP) with 6-311++G(d,p) basis set. The calculated optimized structural parameters and the scaled frequencies are investigated and compared with earlier reported data. The complete vibrational assignment and anal. of the fundamental modes of the mol. were carried out. In addition, mol. electrostatic potential and total electron d. has been analyzed to investigate size, shape, charge d. distribution and site on chem. reactivity of the mol. Finally the Mullikan at. charges of the compound have been studied.

Pharma Chemica published new progress about Atomic charge. 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Recommanded Product: 2-Amino-3-nitro-6-picoline.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Alper, Pinar; Erkisa, Merve; Genckal, Hasene Mutlu; Sahin, Saliha; Ulukaya, Engin; Ari, Ferda published the artcile< Synthesis, characterization, anticancer and antioxidant activity of new nickel(II) and copper(II) flavonoid complexes>, Recommanded Product: 2,2′-Bipyridine, the main research area is nickel copper naringenin quercetin bipyridine terpyridine flavonoid preparation; anticancer antioxidant activity nickel copper flavonoid complex.

Flavonoids are natural products which are known to have biol. activity for human health. In this study, new mixed ligand complexes of Ni(II) and Cu(II) were synthesized by using flavonoid (quercetin or naringenin) and heterocyclic imine (2,2′:6′,2”-terpyridine or 2,2′-bipyridine) ligands. The new complexes are [Ni(narH-1)(terpy)Cl].4H2O (1, nar = naringenin, terpy = 2,2′:6′,2”-terpyridine), [Cu(narH-1)(terpy)Cl].H2O (2), and [Cu(queH-1)(bpy)(O3N)].1.5H2O (3, que = quercetin, bpy = 2,2′-bipyridine). The structural features of the synthesized mixed ligand complexes were investigated using elemental anal., thermogravimetric anal., Fourier transform IR spectroscopy, magnetic susceptibility and molar conductivity measurements. The resulting data demonstrated an octahedral geometry for Complex 1 and Complex 2 and square pyramidal geometry for Complex 3. Antioxidant capacity and total phenolic content of Complexes 1-3 were measured by the Folin-Ciocalteu and ABTS methods. Antiproliferative effect of complexes were tested by SRB and ATP assays on MCF-7 (breast cancer), A549 (nonsmall cell lung cancer), PC-3 (prostate cancer) and HeLa (human cervical cancer) cell lines. Apoptosis was identified using by the fluorescence imaging, caspase cleaved cytokeratin-18 and flow cytometry anal. Complex 2 and 3 had high total phenolic content and antioxidant activity. Complex 2 was found to show selective cytotoxicity through the induction of apoptosis on MCF-7 cells with having a very low IC50 value (<0.8 μM; the half maximum inhibitory concentration) while its ligands showed much higher cytotoxicity (IC50 > 50 μM). In conclusion, Complex 2 is a highly promising and novel compound for breast cancer and warrants further animal experiments

Journal of Molecular Structure published new progress about Antioxidants. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Recommanded Product: 2,2′-Bipyridine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pfefferkorn, Jeffrey A.; Lou, Jihong; Minich, Martha L.; Filipski, Kevin J.; He, Mingying; Zhou, Ru; Ahmed, Syed; Benbow, John; Perez, Angel-Guzman; Tu, Meihua; Litchfield, John; Sharma, Raman; Metzler, Karen; Bourbonais, Francis; Huang, Cong; Beebe, David A.; Oates, Peter J. published the artcile< Pyridones as glucokinase activators: Identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle>, Name: 4,5-Dichloropyridin-2-amine, the main research area is aminopicoline carboxylic acid cyclization transamidation; sulfonyl pyridone preparation glucokinase activation antidiabetic human.

A promising area of novel anti-diabetic therapy involves identification of small mol. activators of the glucokinase enzyme to reduce blood glucose and normalize glucose stimulated insulin secretion. Herein, the identification and optimization of a series of 4-sulfonyl-2-pyridone, i.e. I, activators is reported. The activators were evaluated for in vitro biochem. activation and pharmacokinetic properties. As part of these efforts, a unique metabolic liability of the 4-sulfonyl-2-pyridone ring system was identified wherein this heterocycle readily undergoes conjugation with glutathione under non-enzymic conditions.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 188577-68-6 belongs to class pyridine-derivatives, and the molecular formula is C5H4Cl2N2, Name: 4,5-Dichloropyridin-2-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wagener, Tobias; Heusler, Arne; Nairoukh, Zackaria; Bergander, Klaus; Daniliuc, Constantin G.; Glorius, Frank published the artcile< Accessing (Multi)Fluorinated Piperidines Using Heterogeneous Hydrogenation>, Category: pyridine-derivatives, the main research area is fluoropiperidine diastereoselective preparation; palladium heterogeneous catalyst stereoselective hydrogenation fluoropyridine.

Fluorinated piperidines are desirable motifs for pharmaceutical and agrochem. research. Nevertheless, general synthetic access remains out of reach. Herein, we describe a simple and robust cis-selective hydrogenation of abundant and cheap fluoropyridines to yield a broad scope of (multi)fluorinated piperidines. This protocol enables the chemoselective reduction of fluoropyridines while tolerating other (hetero)aromatic systems using a com. available heterogeneous catalyst. Fluorinated derivatives of important drug compounds are prepared, and a straightforward strategy for the synthesis of enantioenriched fluorinated piperidines is disclosed.

ACS Catalysis published new progress about Aryl fluorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (fluoropyridines). 876919-08-3 belongs to class pyridine-derivatives, and the molecular formula is C7H6FNO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chaubey, Surabhi; Yadav, Rajesh K.; Tripathi, Santosh K.; Yadav, Bal Chandra; Singh, Sudhir N.; Kim, Tae Wu published the artcile< Covalent Triazine Framework as an Efficient Photocatalyst for Regeneration of NAD(P)H and Selective Oxidation of Organic Sulfide>, Product Details of C10H8N2, the main research area is NADPH covalent triazine framework photocatalyst organic sulfide selective oxidation.

Covalent triazine frameworks (CTFs), belonging to the super-family of covalent organic frameworks, have attracted significant attention as a new type of photosensitizer due to the superb light-harvesting ability and efficient charge transfer originating from the large surface area. However, the wide optical band gap in CTFs, which is larger than 3.0 eV, hinders the efficient light harvesting in the visible range. To overcome this limitation, we developed the new type CTFs photocatalyst based on the donor-acceptor conjugation scheme by using melamine (M) and 2,6-diaminoanthraquinone (AQ) as monomeric units. The melamine-2,6-diaminoanthraquinone-based covalent triazine frameworks (M-AQ-CTFs) photocatalyst shows the excellent light-harvesting capacity with high molar extinction coefficient, and the suitable optical band gap involving the internal charge transfer character. Combination of M-AQ-CTFs and artificial photosynthetic system including the organometallic rhodium complex, acting as an electron mediator, exhibited the excellent photocatalytic efficiency for the regeneration of the nicotinamide cofactors such as NAD(P)H. In addition, this photocatalyst showed the high photocatalytic efficiency for the metal-free aerobic oxidation of sulfide. This study demonstrates the high potential of CTFs photocatalyst with the donor-acceptor conjugated scheme can be actively used for artificial photosynthesis.

Photochemistry and Photobiology published new progress about Anaerobic oxidation. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Product Details of C10H8N2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pratap, Ramendra; Yorimitsu, Hideki published the artcile< Palladium-Catalyzed Amination of Aryl Sulfides and Sulfoxides with Azaarylamines of Poor Nucleophilicity>, Recommanded Product: N-Phenylpyridin-4-amine, the main research area is heteroaryl amine preparation; sulfide aryl azaarylamine amination palladium catalyst; sulfoxide aryl azaarylamine amination palladium catalyst.

The amination of aryl sulfides and sulfoxides (Ar)2S and (Ar)2SO2 [Ar = C6H5, 2-naphthyl, biphenyl-4-yl, etc.] with azaarylamines R1NH2 (R1 = pyrimidin-2-yl, pyrazin-2-yl, quinolin-3-yl, etc.) is investigated using a palladium-N-heterocyclic carbene (NHC) complex I. Because azaarylamines are less nucleophilic than anilines, more reactive diaryl sulfides and sulfoxides are found to be suitable coupling partners that liberate better leaving arenethiolate or arenesulfenate anions, instead of aryl Me sulfides RSCH3 [R = 4-FC6H4, 2-naphthyl, 4-(2,5,5-trimethyl-1,3-dioxan-2-yl)phenyl, etc.] as reported previously.

Synthesis published new progress about Amination. 22961-45-1 belongs to class pyridine-derivatives, and the molecular formula is C11H10N2, Recommanded Product: N-Phenylpyridin-4-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Nacsa, Eric D.; MacMillan, David W. C. published the artcile< Spin-Center Shift-Enabled Direct Enantioselective α-Benzylation of Aldehydes with Alcohols>, Formula: C7H6FNO2, the main research area is chiral aldehyde enantioselective preparation; aldehyde alc enantioselective benzylation photoredox organocatalyst photocatalyst.

Nature routinely engages alcs. as leaving groups, as DNA biosynthesis relies on the removal of water from ribonucleoside diphosphates by a radical-mediated “”spin-center shift”” (SCS) mechanism. Alcs., however, remain underused as alkylating agents in synthetic chem. due to their low reactivity in two-electron pathways. We report herein an enantioselective α-benzylation of aldehydes using alcs. as alkylating agents based on the mechanistic principle of spin-center shift. This strategy harnesses the dual activation modes of photoredox and organocatalysis, engaging the alc. by SCS and capturing the resulting benzylic radical with a catalytically generated enamine. Mechanistic studies provide evidence for SCS as a key elementary step, identify the origins of competing reactions, and enable improvements in chemoselectivity by rational photocatalyst design.

Journal of the American Chemical Society published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 876919-08-3 belongs to class pyridine-derivatives, and the molecular formula is C7H6FNO2, Formula: C7H6FNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Shichen; Ren, Jianing; Ding, Chengcheng; Wang, Yishou; Ma, Chen published the artcile< N,N-Dimethylformamide as Carbon Synthons for the Synthesis of N-Heterocycles: Pyrrolo/Indolo[1,2-a]quinoxalines and Quinazolin-4-ones>, Formula: C6H7N3O2, the main research area is pyrroloquinoxaline preparation; aminophenyl pyrrole DMF heterocyclization; indoloquinoxaline preparation; DMF aminophenyl indole heterocyclization; quinazolinone preparation; aminobenzamide DMF heterocyclization.

N,N-dimethylformamide (DMF) as synthetic precursors contributing especially the Me, acyl, and amino groups has played a significant role in heterocycle syntheses and functionalization. In this protocol, a wide range of pyrrolo[1,2-a]quinoxalines I (R = H, Cl, Me; R1 = H, Cl, Me; R2 = H, Cl, F, Br, Me, OMe; R3 = H, Cl, F, Br, Me, CN), II /indolo[1,2-a]quinoxalines III (R4 = H, Cl, Me, CN, etc.; R5 = H, F, Cl, Me) and quinazolin-4-ones IV (R6 = H, 4-Cl, 4-NO2, 5-Fl, 5-Br; R7 = n-Bu, cyclohexyl, Ph, Bn, etc.) were obtained in moderate to good yields by using elemental iodine without any metal or peroxides. N-Me and N-acyl of DMF that participate and complete the reaction sep. through different mechanisms, which displayed potential still to be explored of DMF were considered.

Journal of Organic Chemistry published new progress about Anilines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 21901-29-1 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Formula: C6H7N3O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem