Day: October 21, 2022

Zhang, Lin; Fan, Junhua; Chong, Jer-Hong; Cesena, Angela; Tam, Betty Y. Y.; Gilson, Charles; Boykin, Christina; Wang, Deping; Aivazian, Dikran; Marcotte, Doug; Xiao, Guangqing; Le Brazidec, Jean-Yves; Piao, Jinhua; Lundgren, Karen; Hong, Kevin; Vu, Khang; Nguyen, Khanh; Gan, Liang-Shang; Silvian, Laura; Ling, Leona; Teng, Min; Reff, Mitchell; Takeda, Nicole; Timple, Noel; Wang, Qin; Morena, Ron; Khan, Samina; Zhao, Shuo; Li, Tony; Lee, Wen-Cherng; Taveras, Arthur G.; Chao, Jianhua published the artcile< Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I)>, Related Products of 220731-04-4, the main research area is pyrazolopyrimidine sulfonamide preparation multiple mitotic kinase inhibitor.

A novel class of pyrazolopyrimidine-sulfonamides was discovered as selective dual inhibitors of aurora kinase A (AKA) and cyclin-dependent kinase 1 (CDK1). These inhibitors were originally designed based on an early lead (compound I). SAR development has led to the discovery of potent inhibitors with single digit nM IC50s towards both AKA and CDK1. An exemplary compound II has demonstrated good efficacy in an HCT116 colon cancer xenograft model.

Bioorganic & Medicinal Chemistry Letters published new progress about Alkylation. 220731-04-4 belongs to class pyridine-derivatives, and the molecular formula is C10H15N3O2, Related Products of 220731-04-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fier, Patrick S.; Kim, Suhong; Cohen, Ryan D. published the artcile< A Multifunctional Reagent Designed for the Site-Selective Amination of Pyridines>, Synthetic Route of 3796-23-4, the main research area is Boc protected aminopyridine chemoselective regioselective preparation; pyridine tert butyl chloro dicyanopyrazinyl oxy carbamate amination.

The development of a multifunctional reagent for the direct conversion of pyridines to Boc-protected 2-aminopyridines such as I [R = H, 3-Br, 4-Ph, etc.] with exquisite site selectivity and chemoselectivity was reported. The novel reagent was prepared on 200g scale in a single step, reacted in title reaction under mild conditions without precautions toward air or moisture, and is tolerant of nearly all common functionality. Exptl. and in situ spectroscopic monitoring techniques provided detailed insights and unexpected findings for the unique reaction mechanism.

Journal of the American Chemical Society published new progress about Amination, regioselective (chemoselective). 3796-23-4 belongs to class pyridine-derivatives, and the molecular formula is C6H4F3N, Synthetic Route of 3796-23-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Eastman, Kyle J.; Parcella, Kyle; Yeung, Kap-Sun; Grant-Young, Katharine A.; Zhu, Juliang; Wang, Tao; Zhang, Zhongxing; Yin, Zhiwei; Beno, Brett R.; Sheriff, Steven; Kish, Kevin; Tredup, Jeffrey; Jardel, Adam G.; Halan, Vivek; Ghosh, Kaushik; Parker, Dawn; Mosure, Kathy; Fang, Hua; Wang, Ying-Kai; Lemm, Julie; Zhuo, Xiaoliang; Hanumegowda, Umesh; Rigat, Karen; Donoso, Maria; Tuttle, Maria; Zvyaga, Tatyana; Haarhoff, Zuzana; Meanwell, Nicholas A.; Soars, Matthew G.; Roberts, Susan B.; Kadow, John F. published the artcile< The discovery of a pan-genotypic, primer grip inhibitor of HCV NS5B polymerase>, Application In Synthesis of 777931-67-6, the main research area is hepatitis C virus NS5B polymerase 7 azabenzofuran.

The development of a series of novel 7-azabenzofurans exhibiting pan-genotype inhibition of HCV NS5B polymerase via binding to the primer grip site is presented. Many challenges, including poor oral bioavailability, high clearance, bioactivation, high human serum shift, and metabolic stability were encountered and overcome through SAR studies. This work culminated in the selection of BMS-986139 (43) as a preclin. candidate.

MedChemComm published new progress about Blood serum. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, Application In Synthesis of 777931-67-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fu, Ming-Chen; Shang, Rui; Zhao, Bin; Wang, Bing; Fu, Yao published the artcile< Photocatalytic decarboxylative alkylations mediated by triphenylphosphine and sodium iodide>, Related Products of 350-03-8, the main research area is photocatalytic decarboxylative alkylation triphenylphosphine sodium iodide.

Most photoredox catalysts in current use are precious metal complexes or synthetically elaborate organic dyes, the cost of which can impede their application for large-scale industrial processes. We found that a combination of triphenylphosphine and sodium iodide under 456-nm irradiation by blue light-emitting diodes can catalyze the alkylation of silyl enol ethers by decarboxylative coupling with redox-active esters in the absence of transition metals. Deaminative alkylation using Katritzky’s N-alkylpyridinium salts and trifluoromethylation using Togni’s reagent are also demonstrated. Moreover, the phosphine/iodide-based photoredox system catalyzes Minisci-type alkylation of N-heterocycles and can operate in tandem with chiral phosphoric acids to achieve high enantioselectivity in this reaction.

Science (Washington, DC, United States) published new progress about Acid catalysis (chiral Bronsted acid). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Related Products of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gujjarappa, Raghuram; Vodnala, Nagaraju; Musib, Dulal; Malakar, Chandi C. published the artcile< Organocatalytic Decarboxylation and Dual C(sp3)-H Bond Functionalization Toward Facile Access to Divergent 2,6-Diarylpyridines>, Electric Literature of 350-03-8, the main research area is diarylpyridine preparation; ketone amino acid decarboxylation proline catalyst.

An effective organocatalytic protocol toward the assembly of sym. and unsym. 2,6-diarylpyridines I (R1 = H, Me, CN; R2 = Ph, 4-methylphenyl, 2H-1,3-benzodioxol-5-yl, etc.; R3 = Ph, 4-nitrophenyl, pyridin-3-yl, etc.) is demonstrated. The reaction proceeds through organocatalytic decarboxylation of amino acids R4CH(NH2)C(O)OH and dual C(sp3)-H bond oxidation of carbonyl compounds R1CH2C(O)R2 and R1CH2C(O)R3. Catalyst screening revealed that explicit choice of L-proline could lead to the formation of product with maximum yield and selectivity. The developed process appears with operational simplicity and is consistent with broad range of functional groups.

Asian Journal of Organic Chemistry published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Electric Literature of 350-03-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Xie, Demeng; Wang, Yingwei; Zhang, Xia; Fu, Zhengyan; Niu, Dawen published the artcile< Alkyl/Glycosyl Sulfoxides as Radical Precursors and Their Use in the Synthesis of Pyridine Derivatives>, COA of Formula: C6H4F3N, the main research area is pyridine alkyl regioselective preparation; alkyl glycosyl sulfoxide regioselective stereoselective photochem alkylation methoxypyridinium; Alkyl Sulfoxides; C-Glycosides; Electron Donor-Acceptor Complexes; Photochemistry; Radicals.

Here the use of simple and readily available alkyl sulfoxides as precursors to radicals and their application in the preparation of pyridine derivatives are reported. It was shown that alkyl sulfoxides, N-methoxy pyridinium salts and fluoride anions form electron donor-acceptor (EDA) complexes in solution, which, upon visible light irradiation, undergo a radical chain process to afford various pyridine derivatives smoothly. This reaction displays broad scope with respect to both sulfoxides and N-methoxy pyridinium salts. The synthetic versatility of sulfoxides as a handle in chem. adds to their power as radical precursors. Glycosyl sulfoxides are converted to the corresponding pyridyl C-glycosides with high stereoselectivities. Computational and exptl. studies provide insights into the reaction mechanism.

Angewandte Chemie, International Edition published new progress about Alkylation, regioselective. 3796-23-4 belongs to class pyridine-derivatives, and the molecular formula is C6H4F3N, COA of Formula: C6H4F3N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Park, Eunsun; Lee, Sun Joo; Moon, Heegyum; Park, Jongmi; Jeon, Hyeonho; Hwang, Ji Sun; Hwang, Hayoung; Hong, Ki Bum; Han, Seung-Hee; Choi, Sun; Kang, Soosung published the artcile< Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors>, Formula: C8H5ClN2O2, the main research area is methyl pyrrolopyridine carboxamide preparation Janus kinase inhibitor mol docking.

Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Anal. of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamides I (R = H, Me, cyclopropyl, cyclopentyl) as a JAK1-selective scaffold, and the synthesis of various Me amide derivatives e.g., II, provided III as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of III exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of III on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-β-induced hepatic stellate cells (HSCs). Specifically, III significantly inhibited TGF-β-induced migration of HSCs at 0.25μM in wound-healing assays.

Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 920966-03-6 belongs to class pyridine-derivatives, and the molecular formula is C8H5ClN2O2, Formula: C8H5ClN2O2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kanizaj, Lidija; Molcanov, Kresimir; Toric, Filip; Pajic, Damir; Loncaric, Ivor; Santic, Ana; Juric, Marijana published the artcile< Ladder-like [CrCu] coordination polymers containing unique bridging modes of [Cr(C2O4)3]3- and Cr2O72->, Application In Synthesis of 366-18-7, the main research area is crystal structure copper oxalate chromium dichromate diimine coordination polymer; copper oxalate chromium dichromate diimine polymer preparation antiferromagnetic.

Three heterometallic 1-dimensional (1D) coordination polymers {A[CrCu2(bpy)2(C2O4)4]·H2O}n [A = K+ 1 and NH4+ 2; bpy = 2,2′-bipyridine] and [(Cr2O7)Cu2(C2O4)(phen)2]n (3; phen = 1,10-phenanthroline) with uncommon topol. were synthesized using a building block approach and characterized by single-crystal x-ray diffraction, IR and impedance spectroscopies, magnetization measurements, and DFT calculations Due to the partial decomposition of the building block [Cr(C2O4)3]3-, all three compounds contain oxalate-bridged [Cu2(L)2(μ-C2O4)]2+ units [L = bpy 1 and 2 and phen 3]. In compounds 1 and 2, these cations are mutually connected through oxalate groups from [Cr(C2O4)3]3-, thus forming ladder-like topologies. Unusually, three different bridging modes of the oxalate ligand are observed in these chains. In compound 3 Cu(II) ions from cationic units are bridged through the O atoms of Cr2O72- anions in a novel ladder-like mode. Very strong antiferromagnetic coupling observed in all three compounds, determined from the magnetization measurements and confirmed by DFT calculations (J = -343, -371 and -340 cm-1 for 1-3, resp.), appears between two Cu(II) ions interacting through the oxalate bridge.

Dalton Transactions published new progress about Antiferromagnetic exchange. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Application In Synthesis of 366-18-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gallou, Fabrice; Reeves, Jonathan T.; Tan, Zhulin; Song, Jinhua J.; Yee, Nathan K.; Harcken, Christian; Liu, Pingrong; Thomson, David; Senanayake, Chris H. published the artcile< Practical regioselective bromination of azaindoles and diazaindoles>, Reference of 23612-36-4, the main research area is azaindole regioselective bromination copper bromide; diazaindole regioselective bromination; brominated azaindole preparation; pyridine pyrrolo bromo preparation; pyridazine pyrrolo bromo preparation.

A mild and efficient synthesis of various 3-brominated azaindoles and diazaindoles was developed by regioselective halogenation of the parent systems. This practical and high-yielding transformation was achieved with copper(II) bromide in acetonitrile at room temperature

Synlett published new progress about Bromination, regioselective. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, Reference of 23612-36-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Shuguang; Chen, Liang; Zhou, Xiaojun; Sun, Ping; Fu, Liwen; You, Yanling; Xu, Man; You, Zhengwei; Kai, Guoyin; He, Chuanglong published the artcile< Tumor-targeted biodegradable multifunctional nanoparticles for cancer theranostics>, Category: pyridine-derivatives, the main research area is tumor targeting biodegradable multifunctional nanoparticle cancer theranostic.

Mesoporous silica nanoparticles (MSN) attract extensive attention in area of cancer diagnosis and therapy because of their controllable nanostructures, easy surface modification and stable synthesis methods. However, their biodegradability was still controversial. This work explored the degradation effect of a type of biodegradable MSN (bMSN) in different environments and simultaneously endowed it with imaging functions and high-efficiency targeting effect on cancer cell, thus forming a multifunctional biodegradable drug carrier (bMSN-ss-GABA) for cancer theranostics. The bovine serum albumin-based Gd/Au complex (BSA-Gd/Au) was wrapped on the surface of bMSN through disulfide linkage, acting as contrast agent for magnetic resonance (MR) and fluorescence imaging, and then folate (FA), whose receptor (FR) is overexpressed in KB human oral epidermoid carcinoma cells, was modified on the nanocarriers as a targeting ligand. TEM revealed the degradation process of bMSN and a series of characterization methods verified the successful construction of bMSN-ss-GABA. Doxorubicin hydrochloride (DOX) loaded bMSN-ss-GABA (DOX@bMSN-ss-GABA) was proved with redox-responsiveness, thereby triggering rapid drug release under specific tumor microenvironment of high glutathione concentration Further, the excellent imaging capability was also fully inspected. What’s more, the results of endocytosis and tumor growth inhibition of DOX@bMSN-ss-GABA demonstrated the highly effective targeting effect of hybrid nanocarriers. Therefore, the prepared DOX@bMSN-ss-GABA might be used as a promising nanotheranostic agent for KB human oral epidermoid carcinoma.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem