Day: October 21, 2022

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

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

Looga, A. M.; Ambassa, P.; Kamga, J.; Hortense, GK.; Ngadjui, B. T.; Ngameni, B. published the artcile< Synthesis and evaluation of antimicrobial properties of some novel indole pyridine based chalcones>, SDS of cas: 350-03-8, the main research area is chalcone indole pyridine diastereoselective preparation antibacterial antifungal; indolyl pyridinyl propenone preparation diastereoselective antibacterial antifungal activity.

A series of novel substituted indolylchalcone derivatives (E)-I (R = H, Me, Ar = pyridin-3-yl, pyridin-4-yl) were synthesized via Claisen-Schmidt condensation between indole-3-carbaldehyde and N-methylindole-3-carbaldehyde and 3- and 4-pyridinylacetophenones. All the compounds were screened for their antibacterial and antifungal activity against six different bacterial strains – Escherichia coli ATCC 25922, Klebsiella pneumonia ATCC 700603, Staphylococcus aureus ATCC 25923, Proteus mirabilis, Salmonella typhi, Pseudomonas aeruginosa – and against one fungal strain, Candida albicans. The results reveal that all the compounds exhibited moderate to good antibacterial and antifungal activities.

Austin Journal of Analytical and Pharmaceutical Chemistry published new progress about Antibacterial agents. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, SDS of cas: 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gao, Li; Wu, Datong; Tan, Wensheng; Pan, Fei; Xu, Jiale; Tao, Yongxin; Kong, Yong published the artcile< A facile synthesis of two ionized fluorescent carbon dots and selective detection toward Fe2+ and Cu2+>, Name: Pyridin-4-ylmethanamine, the main research area is iron copper carbon dot selective detection.

In this study, a facile synthesis of two ionized carbon dots (CDs-2 and CDs-3) is reported, in which different ionic pairs are formed at the surface of the carbon core. In contrast to CDs-3, the accumulation of carbon core can be clearly observed in the TEM image of CDs-2. This is due to the linkage of the dibromine alkyl group. Compared with naked CDs in the absence of the ionic pair, the maximum emission wavelength undergoes a red-shift of nearly 60 nm. Moreover, protic solvents (water, ethanol and N,N′-dimethyl formamide) have an apparent effect on the emission intensities of CDs-2 and CDs-3. The time-resolved average lifetimes of CDs-2 and CDs-3 are calculated as 56.34 ns and 54.50 ns, resp. Furthermore, they both have much better fluorescence stability in the solution with pH ranging from 2 to 11 due to the presence of the imidazolium cation. It is interesting to see that CDs-2 and CDs-3 have much different responses towards Cu2+ and Fe2+. The CDs-3 solution generates clear fluorescence quenching when treated with Fe2+. In brief, we believe that these findings can inspire more research developments in the synthesis and further application of functional CDs.

Nanoscale Advances published new progress about Carbon quantum dots. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Name: Pyridin-4-ylmethanamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Beller, Matthias; Magerlein, Wolfgang; Indolese, Adriano F.; Fischer, Christine published the artcile< Efficient palladium-catalyzed alkoxycarbonylation of N-heteroaryl chlorides - A practical synthesis of building blocks for pharmaceuticals and herbicides>, Formula: C6H6ClNO, the main research area is butyl pyridinecarboxylate preparation; heteroaryl chloride alkoxycarbonylation palladium phosphine ligand catalyst; alkoxycarbonylation chloropyridine palladium catalyst.

The alkoxycarbonylation of various N-heteroaryl chlorides was examined in detail. Studies of the butoxycarbonylation of 2- and 3-chloropyridine revealed the importance of selecting both the right phosphine ligand and ligand concentration in order to obtain efficient conversion and selectivity. Amongst the different ligands tested, 1,4-bis(diphenylphosphino)butane (dppb) and 1,1′-bis(diphenylphosphino)ferrocene (dppf) led to the most efficient palladium catalyst systems for the conversion of 2- and 4-chloropyridines and similar heteroaryl chlorides. For e.g., Bu pyridine-2-carboxylate was prepared in 95% yield in the presence of dppf ligand. The best catalytic systems for the alkoxycarbonylation of less activated substrates, such as 3-chloropyridines, were found to be those containing 1,4-bis(dicyclohexylphosphino)butane. Good to excellent yields of a number of N-heterocyclic carboxylic acid esters were realized by applying the appropriate ligand in the right concentration at low catalyst loadings (0.005-0.5 mol% Pd). For the first time catalyst turnover numbers (TON) of up to 13,000 were obtained for the carbonylation of a (hetero)aryl chloride.

Synthesis published new progress about Alkoxycarbonylation. 13472-84-9 belongs to class pyridine-derivatives, and the molecular formula is C6H6ClNO, Formula: C6H6ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhou, Bo; Wang, Yang; Yan, Yiwu; Mariscal, Javier; Di Vizio, Dolores; Freeman, Michael R.; Yang, Wei published the artcile< Low-Background Acyl-Biotinyl Exchange Largely Eliminates the Coisolation of Non-S-Acylated Proteins and Enables Deep S-Acylproteomic Analysis>, HPLC of Formula: 2127-03-9, the main research area is acyl biotinyl exchange S acylated protein proteomic.

Protein S-acylation (also called palmitoylation) is a common post-translational modification whose deregulation plays a key role in the pathogenesis of many diseases. Acyl-biotinyl exchange (ABE), a widely used method for the enrichment of S-acylated proteins, has the potential of capturing the entire S-acylproteome in any type of biol. sample. Here, we showed that current ABE methods suffer from a high background arising from the coisolation of non-S-acylated proteins. The background can be substantially reduced by an addnl. blockage of residual free cysteine residues with 2,2′-dithiodipyridine prior to the biotin-HPDP reaction. Coupling the low-background ABE (LB-ABE) method with label-free proteomics, 2 895 high-confidence candidate S-acylated proteins (including 1 591 known S-acylated proteins) were identified from human prostate cancer LNCaP cells, representing so-far the largest S-acylproteome data set identified in a single study. Immunoblotting anal. confirmed the S-acylation of five known and five novel prostate cancer-related S-acylated proteins in LNCaP cells and suggested that their S-acylation levels were about 0.6-1.8%. In summary, the LB-ABE method largely eliminates the coisolation of non-S-acylated proteins and enables deep S-acylproteomic anal. It is expected to facilitate a much more comprehensive and accurate quantification of S-acylproteomes than previous ABE methods.

Analytical Chemistry (Washington, DC, United States) published new progress about Mammalian cell. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, HPLC of Formula: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Yue; Jiang, Zhensheng; Li, Zhihong; Gu, Jing; You, Qidong; Zhang, Xiaojin published the artcile< Click Chemistry-Based Discovery of [3-Hydroxy-5-(1H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia>, Synthetic Route of 870997-85-6, the main research area is preparation hydroxytriazolyl picolinoyl glycine derivative HIF PHD2 inhibitor anemia.

As a gene associated with anemia, the erythropoiesis gene is physiol. expressed under hypoxia regulated by †hypoxia-inducing factor-α (HIF-α). Thus, stabilizing HIF-α is a potent strategy to stimulate the expression and secretion of erythropoiesis. In this study, we applied click chem. to the discovery of HIF prolyl hydroxylase 2 (HIF-PHD2) inhibitors for the first time, and a series of triazole compounds showed preferable inhibitory activity in fluorescence polarization assays. Of particular note was the orally active HIF-PHD inhibitor 15i (IC50 = 62.23 nM), which was almost ten times more active than the phase III drug FG-4592 (IC50 = 591.4 nM). Furthermore, it can upregulate the Hb of cisplatin-induced anemia mice (120 g/L) to normal levels (160 g/L) with no apparent toxicity observed in vivo. These results confirm that triazole compound 15i is a promising candidate for the treatment of renal anemia.

Journal of Medicinal Chemistry published new progress about Anemia. 870997-85-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrN2O2, Synthetic Route of 870997-85-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mizukawa, Yuki; Ikegami-Kawai, Mayumi; Horiuchi, Masako; Kaiser, Marcel; Kojima, Masayoshi; Sakanoue, Seiki; Miyagi, Seiya; Nanga Chick, Christian; Togashi, Hiroyuki; Tsubuki, Masayoshi; Ihara, Masataka; Usuki, Toyonobu; Itoh, Isamu published the artcile< Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines>, Reference of 3731-53-1, the main research area is dimethoxyquinazolinediamine preparation antimalarial; Antimalarial drug; Derivatization; Quinazoline-2,4-diamines; SAR.

Quinazolines have long been known to exert varied pharmacol. activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, author’s have synthesized approx. 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies. Here, author’s summarize the results and report the discovery of 6,7-dimethoxy-N4-(1-phenylethyl)-2-(pyrrolidin-1-yl)quinazolin-4-amine, which exhibits high antimalarial activity as a promising antimalarial drug lead.

Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Reference of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Xiaoyue; Ye, Weidong; Song, Xiaohua; Ma, Wenxin; Lao, Xuejun; Shen, Runpu published the artcile< Novel ionic liquid with both Lewis and Bronsted acid sites for Michael addition>, Reference of 21876-43-7, the main research area is ionic liquid Lewis Bronsted acid preparation Michael addition; Lewis and Brønsted acid sites; Michael addition; novel ionic liquid.

Ionic liquid with both Lewis and Bronsted acid sites has been synthesized and its catalytic activities for Michael addition were carefully studied. The novel ionic liquid was stable to water and could be used in aqueous solution The molar ratio of the Lewis and Bronsted acid sites could be adjusted to match different reactions. The results showed that the novel ionic liquid was very efficient for a Michael addition and the synthesis of the target compounds was achieved in good to excellent yield within several min. Operational simplicity, high stability to water and air, small amount used, low cost of the catalyst used, high yields, chemoselectivity, applicability to large-scale reactions and reusability are the key features of this methodol., which indicated that this novel ionic liquid also holds great potential for environmentally friendly processes (green chem. methods).

International Journal of Molecular Sciences published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Reference of 21876-43-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem