Day: December 9, 2022

Liang, Ren-Xiao published the artcileEnantioselective Arylation of Tetrasubstituted Enamines: Access to Enantioenriched Indolenine and 1H-Indole Derivatives, Application of 2-Bromopyridin-3-amine, the publication is ACS Catalysis (2021), 11(3), 1827-1832, database is CAplus.

Palladium-catalyzed intramol. enantioselective β-arylation of tetrasubstituted endocyclic and exocyclic enamines was developed. A range of optically active medium-ring fused indolenines or 3,3′-spiroindolenines were achieved in enantiomeric ratios up to 98:2 with Cs₂CO₃ or K₃PO₄ as the base in the presence of chiral PHOX ligands. The use of Ag₃PO₄ as a base led to enantioenriched 1H-indoles in good enantiomeric ratios (up to 89:11) with (S)-DIFLUORPHOS as a chiral ligand, which proceeded via a possible domino enamine-isomerization/β-arylation sequence.

ACS Catalysis published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Application of 2-Bromopyridin-3-amine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Obdyakov, V. F. published the artcileStabilization of palladium in homogeneous chlorideless catalysts of oxidation of olefins C₂-C₄ by oxygen into carbonyl compounds, HPLC of Formula: 636-73-7, the publication is Kataliz v Promyshlennosti (2007), 19-25, database is CAplus.

The first step of homogeneous oxidation of olefins C₂-C₄ by oxygen in the presence of catalyst Pd + GPK-x, were GPK-x is phosphovanadomolybdic heteropoly acid H_3+xPV^V_x Mo_12-xO₄₀, consist in reduction of GPK-x with olefin in the presence Pd-complexes at 30-60° into H_mGPK-x where m=[V^IV]_∑/[GKP-x] – is excellent reduction catalyst. In this case the redox-system Pd¹₂/Pd⁰₂ works and with increasing of temperature in converts into system Pd²⁺/Pd_MET with higher redox-potential. During this transformation interval of values m is diminished where the catalyst remained as homogeneous and from reduced solution metallic Pd begins to precipitate To prevent the Pd precipitation it needs to introduce in catalyst the stabilizers stable from oxidation As stabilizers can be used 3-pyridinesulfonic acid of more cheaper 2,6-pyridinecarboxylic (dipicolinic) acid (I). In the presence of the stabilizers the activity of catalyst is diminished but the area of its homogeneity will extend. Complexes of Pd with I are stable at temperatures of regeneration of catalyst (150-160°). Therefore I is considered as rather perspective stabilizer of Pd in catalysts Pd + GPK-x and can be used in industrial homogeneous processes of oxidation of olefins C₂-C₄ with oxygen.

Kataliz v Promyshlennosti published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, HPLC of Formula: 636-73-7.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wu, De-Zhi published the artcileAn efficient method for the construction of 2-Aminothiazolo[5,4-c]pyridines via K₃[Fe(CN)₆] oxidized SP² C-H Functionalization, Computed Properties of 18437-58-6, the publication is Tetrahedron (2016), 72(52), 8610-8616, database is CAplus.

A practical approach to synthesize 2-aminothiazolo[5,4-c]pyridines from simple asym. pyridylthioureas was achieved by utilizing K₃[Fe(CN)₆] as the oxidant [e.g., I → II (97%)]. These reactions went through an intramol. oxidation and finally led to the formation of C-S bond. Furthermore, the possible oxidative cyclization mechanism was also explored by the addition of radical scavengers, which showed that the oxidative cyclization was promoted via a free radical mechanism.

Tetrahedron published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C7H16Cl2Si, Computed Properties of 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Benyettou, Farah published the artcileRedox-Responsive Viologen-Mediated Self-Assembly of CB[7]-Modified Patchy Particles, Formula: C22H18Cl2N2, the publication is Langmuir (2016), 32(28), 7144-7150, database is CAplus and MEDLINE.

Sulfonated surface patches of poly(styrene)-based colloidal particles (CPs) were functionalized with cucurbit[7]uril (CB[7]). The macrocycles served as recognition units for di-Ph viologen (DPV²⁺), a rigid bridging ligand. The addition of DPV²⁺ to aqueous suspensions of the particles triggered the self-assembly of short linear and branched chainlike structures. The self-assembly mechanism is based on hydrophobic/ion-charge interactions that are established between DPV²⁺ and surface-adsorbed CB[7]. DPV²⁺ guides the self-assembly of the CPs by forming a ternary DPV²⁺⊂(CB[7])₂ complex in which the two CB[7] macrocycles are attached to two different particles. Viologen-driven particle assembly was found to be both directional and reversible. Whereas sodium chloride triggers irreversible particle disassembly, the one-electron reduction of DPV²⁺ with sodium dithionite causes disassembly that can be reversed via air oxidation Thus, this bottom-up synthetic supramol. approach allowed for the reversible formation and directional alignment of a 2D colloidal material.

Langmuir published new progress about 47369-00-6. 47369-00-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Salt,Benzene,Organic ligands for MOF materials,Nitrogen containing MOF ligands,Nitrogen containing MOF ligands, name is 1,1′-Diphenyl-[4,4′-bipyridine]-1,1′-diium chloride, and the molecular formula is C22H18Cl2N2, Formula: C22H18Cl2N2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wang, JiaoYang published the artcileComputational study on C-B homolytic bond dissociation enthalpies of organoboron compounds, Application of 2-Pyridinylboronic acid, the publication is New Journal of Chemistry (2017), 41(3), 1346-1362, database is CAplus.

Based on many transition-metal-catalyzed Suzuki-Miyaura cross-coupling reactions of organoboron compounds in which C-B cleavages are involved, it is meaningful to understand one of the thermodn. properties of the C-B bond, the strength of the C-B bond, which can be measured using homolytic bond dissociation enthalpies (BDEs). To this end, we first calculated 64 C-B BDEs of organoboron compounds by theor. methods including composite high-level ab initio methods of G3, G4, G3B3, CBS-Q, CBS-QB3, and CBS-4M and 34 d. functional theory (DFT) methods. The results show that it is reasonable and credible to regard the average values of six composite high-level methods as the standard C-B BDE values. By comparing the DFT methods, it is found that the M06-HF method provides the most accurate results and the root mean square error (RMSE) is the smallest of 6.4 kJ mol^-1. Therefore, the C-B BDEs including C(sp)-B, C(sp²)-B and C(sp³)-B of organoboron compounds such as boronic acids, trifluoroborate salts, boronate esters, etc. as well as the substituent effects were investigated by using the M06-HF method. The results indicated that the different substituents including electron-donating groups (EDGs), electron-withdrawing groups (EWGs) and conjugated effect groups (CEGs) exhibit different effects on different types of C-B BDEs. Moreover, the natural bond orbital (NBO) anal. was performed in order to further disclose the essence of BDE change patterns.

New Journal of Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C15H20O6, Application of 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Yuan, Chunling published the artcileCu(II)-catalyzed homocouplings of (hetero)arylboronic acids with the assistance of 2-O-methyl-D-glucopyranose, COA of Formula: C5H6BNO2, the publication is Molecules (2019), 24(20), 3678pp., database is CAplus and MEDLINE.

This is the first report of a natural ligand improving the copper-catalyzed homocouplings of (hetero)arylboronic acids. Various important synthetic biaryl intermediates in organic synthesis could be assembled via this method. To gain insight into this reaction, in-situ React IR technol. was used to confirm the effectivity of this catalyst system. This protocol provides important biaryl compounds in high yields within a short time.

Molecules published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C6H16OSi, COA of Formula: C5H6BNO2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Li, Yan published the artcilePotassium tert-butoxide promoted regioselective deuteration of pyridines, Formula: C13H13N, the publication is Chemical Communications (Cambridge, United Kingdom) (2022), 58(21), 3497-3500, database is CAplus and MEDLINE.

A regioselective deuteration at the β- and γ-position of pyridines was reported. Efficient deuteration occurred with a combination of KO^tBu and DMSO-d₆, replenishing the prevailing α-deuteration of the pyridine systems. Preliminary mechanistic studies suggested that the dimsyl carbanion acts as one of the key intermediates.

Chemical Communications (Cambridge, United Kingdom) published new progress about 85237-71-4. 85237-71-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is 5-Methyl-2-(p-tolyl)pyridine, and the molecular formula is C13H13N, Formula: C13H13N.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wolkenberg, Scott E. published the artcileDesign, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2, Recommanded Product: (6-Hydroxypyridin-3-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2011), 54(7), 2351-2358, database is CAplus and MEDLINE.

Agonists of somatostatin receptor subtype 2 (sst₂) have been proposed as therapeutics for the treatment of proliferative diabetic retinopathy and exudative age-related macular degeneration. An HTS screen identified 2-quinolones as weak agonists of sst₂, and these were optimized to provide small mols. with sst₂ binding and functional potency comparable to peptide agonists. Agonist I was shown to inhibit rat growth hormone secretion following systemic administration and to inhibit ocular neovascular lesion formation after local administration.

Journal of Medicinal Chemistry published new progress about 903899-13-8. 903899-13-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Alcohol,Boronic Acids,Boronic acid and ester, name is (6-Hydroxypyridin-3-yl)boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: (6-Hydroxypyridin-3-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zhang, Yong published the artcileDiscovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents, HPLC of Formula: 39856-58-1, the publication is ACS Medicinal Chemistry Letters (2018), 9(11), 1117-1122, database is CAplus and MEDLINE.

The multi-functional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and durable immune response against tumors. Herein, we describe a novel series of 4-azaindole TGFβ receptor kinase inhibitors with excellent selectivity for TGFβ receptor 1 kinase. The combination of compound 3f and an antimouse-PD-1 antibody demonstrated significantly improved antitumor efficacy compared to either treatment alone in a murine tumor model.

ACS Medicinal Chemistry Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C39H35N5O8, HPLC of Formula: 39856-58-1.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Xin, Minhang published the artcileSynthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton’s tyrosine kinase (BTK) inhibitors, COA of Formula: C10H18BNO4, the publication is Bioorganic & Medicinal Chemistry (2015), 23(19), 6250-6257, database is CAplus and MEDLINE.

A series of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines I [R¹ = piperidin-3-yl, piperidin-4-yl, 1,2,3,6-tetrahydropyridin-4-yl, etc.] as potent BTK inhibitors were designed, synthesized and evaluated. These thieno[3,2-c]pyridin-4-amine derivatives displayed variant inhibitory activities against BTK in vitro. Among these, 7-pyrazol-4-yl substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amine subseries showed high BTK inhibition and several compounds displayed superior BTK inhibitory activity. Comprehensive SAR was disclosed and compound I [R¹ = 1-morpholinoethanoe-2-yl] showed excellent potency (IC₅₀ = 11.8 nM), outstanding hydrophilicity (A log P = 3.53), and relatively good kinase selectivity, being a promising lead for further evaluation.

Bioorganic & Medicinal Chemistry published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C9H6N2O2, COA of Formula: C10H18BNO4.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem