Month: October 2022

Shrimp, Jonathan H.; Jing, Yihang; Gamage, Supuni Thalalla; Nelson, Kathryn M.; Han, Joseph; Bryson, Keri M.; Montgomery, David C.; Thomas, Justin M.; Nance, Kellie D.; Sharma, Sunny; Fox, Stephen D.; Andressen, Thorkell; Sinclair, Wilson R.; Wu, Hong; Allali-Hassani, Abdellah; Senisterra, Guillermo; Vedadi, Masoud; Lafontaine, Denis; Dahlin, Jayme L.; Marmorstein, Ronen; Walters, Michael A.; Meier, Jordan L. published the artcile< Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation>, Computed Properties of 20099-90-5, the main research area is remodelin cryptic assay interference chemotype NAT10 acetylase RNA acetylation.

Remodelin is a putative small mol. inhibitor of the RNA acetyltransferase NAT10 which has shown preclin. efficacy in models of the premature aging disease Hutchinson-Gilford Progeria Syndrome (HGPS). Here we evaluate remodelin’s assay interference characteristics and effects on NAT10-catalyzed RNA cytidine acetylation. We find the remodelin chemotype constitutes a cryptic assay interference compound, which does not react with small mol. thiols but demonstrates protein reactivity in ALARM NMR and proteome-wide affinity profiling assays. Biophys. analyses find no direct evidence for interaction of remodelin with the NAT10 acetyltransferase active site. Cellular studies verify that N4-acetylcytidine (ac4C) is a nonredundant target of NAT10 activity in human cell lines and find that this RNA modification is not affected by remodelin treatment in several orthogonal assays. These studies display the potential for remodelin’s chemotype to interact with multiple protein targets in cells and indicate remodelin should not be applied as a specific chem. inhibitor of NAT10-catalyzed RNA acetylation.

ACS Medicinal Chemistry Letters published new progress about Homo sapiens. 20099-90-5 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO3, Computed Properties of 20099-90-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Nikitine, Serge published the artcile< Anisotropic absorption of different radiations by some dyes>, Recommanded Product: 4-Bromoisobenzofuran-1,3-dione, the main research area is .

The photodichroism, after insolation in white light polarized rectilinearly, of several dyes (cyanine, pinacyanol, etc.) is measured as a function of λ.

Compt. rend. published new progress about Dichroism. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Recommanded Product: 4-Bromoisobenzofuran-1,3-dione.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hong, Liang; Liu, Chunxia; Sun, Wangsheng; Wang, Lei; Wong, Kwokyin; Wang, Rui published the artcile< Organocatalytic Enantioselective Friedel-Crafts Alkylation of 4,7-Dihydroindoles with α,β-Unsaturated Aldehydes: An Easy Access to 2-Substituted Indoles>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is dihydroindole unsaturated aldehyde chiral diarylprolinol trimethylsilyl ether; enantioselective Friedel Crafts alkylation benzoquinone oxidation; substituted dihydroindole indole stereoselective preparation; Friedel Crafts alkylation enantioselective catalyst chiral diarylprolinol trimethylsilyl ether.

An enantioselective Friedel-Crafts alkylation of 4,7-dihydroindoles and α,β-unsaturated aldehydes has been developed. The process is promoted by diphenylprolinol ether to afford 2-substituted 4,7-dihydroindoles, e.g., I, in high yields and enantioselectivities. After a subsequent oxidation of the products, the optically active 2-substituted indoles could be obtained smoothly in high yields without any loss of enantioselectivity.

Organic Letters published new progress about Friedel-Crafts reaction (enantioselective). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wang, Tao; Chen, Xuling; Li, Pengfei published the artcile< One-Pot Divergent Synthesis of Benzoxazines and Dihydroquinolines from Morita-Baylis-Hillman Alcohols>, Quality Control of 20776-50-5, the main research area is hydroxy carboxypropylene benzamide intramol heterocyclization; carboxyethylene benzoxazine preparation; acyl dihydroquinoline carboxylate preparation.

Benzoxazines and hydroquinolines was prepared by a one-pot process via catalyst-controlled divergent annulations of Morita-Baylis-Hillman (MBH) alcs. In the presence of diazabicyclo[2.2.2]octane, MBH alcs. reacted with Boc2O to form MBH carbonates, followed by intramol. annulation to give 4H-benzo[d][1,3]oxazines. Divergently, the combination of Bu4NBr and NaOH enabled the formation of 1,2-dihydroquinolines from the same starting materials.

European Journal of Organic Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Quality Control of 20776-50-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Du, Shaoqing; Hu, Xueping; Shao, Xusheng; Qian, Xuhong published the artcile< Novel trifluoromethyl sydnone derivatives: Design, synthesis and fungicidal activity>, Recommanded Product: 4-Bromobenzylamine, the main research area is trifuoromethyl sydnone derivative preparation antifungal; Antifungal; Mesoionic; Sydnone; Trifluoromethyl.

In this study, a series of noval sydnone mesoionic derivatives I (R1 = H, Ph, 3-trifluoromethylphenyl, 3,5-dichlorophenyl; R2 = 3-trifluoromethylphenyl, tetrahydrofuran-2-yl, cylcopropyl, etc.) by active substructure splicing were designed and synthesized. All compounds were characterized using 1H and 13C NMR spectroscopy. Among them, trifluoromethyl compound I (R1 = R2 = 3-trifluoromethylphenyl) showed good bioactivity against Pseudoperonospora cubensis (EC50 = 49 mg L-1) in vivo, the activity was similar to that of the control Kresoxim-Me (EC50 = 44 mg L-1). However, the target of these compounds should not only be tyrosinase, and the mode of action needs to be further studied. In addition, the structure-activity relationship indicated that the trifluoromethyl group was more beneficial for antifungal activity. This is the first report that fluorine-containing N(3)-benzyl sydnone compounds have good fungicidal activity. These results will provide a basis for the development of sydnone mesoionic as new lead fungicidal agents.

Bioorganic & Medicinal Chemistry Letters published new progress about Agrochemical fungicides. 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Recommanded Product: 4-Bromobenzylamine.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chu, John C. K.; Dalton, Derek M.; Rovis, Tomislav published the artcile< Zn-Catalyzed Enantio- and Diastereoselective Formal [4 + 2] Cycloaddition Involving Two Electron-Deficient Partners: Asymmetric Synthesis of Piperidines from 1-Azadienes and Nitro-Alkenes>, Related Products of 16426-64-5, the main research area is zinc catalyst stereoselective formal cycloaddition azadiene nitroalkene kinetics; stereoselective preparation piperidine.

We report a catalytic asym. synthesis of piperidines, e.g. I, through [4 + 2] cycloaddition of 1-azadienes and nitro-alkenes. The reaction uses earth abundant Zn as catalyst and is highly diastereo- and regioselective. A novel BOPA ligand (F-BOPA) confers high reactivity and enantioselectivity in the process. The presence of ortho substitution on the arenes adjacent to the bis(oxazolines) was found to be particularly impactful, due to limiting the undesired coordination of 1-azadiene to the Lewis acid and thus allowing the reaction to be carried out at lower temperature A series of secondary kinetic isotope effect studies using a range of ligands implicates a stepwise mechanism for the transformation, involving an initial Michael-type addition of the imine to the nitro-alkene followed by a cyclization event. The stepwise mechanism obviates the electronic requirement inherent to a concerted mechanism, explaining the successful cycloaddition between two electron-deficient partners.

Journal of the American Chemical Society published new progress about [4+2] Cycloaddition reaction (formal stereoselective). 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Related Products of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Bing; Hu, Jiantao; Xu, Fuming; Chen, Zhuo; Bai, Longchuan; Fernandez-Salas, Ester; Lin, Mei; Liu, Liu; Yang, Chao-Yie; Zhao, Yujun; McEachern, Donna; Przybranowski, Sally; Wen, Bo; Sun, Duxin; Wang, Shaomeng published the artcile< Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression>, Related Products of 82-73-5, the main research area is preparation degrader bromodomain extra terminal protein cancer.

The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “”readers”” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive therapeutic targets for cancer and other human diseases. Recently, heterobifunctional small-mol. BET degraders have been designed based upon the proteolysis targeting chimera (PROTAC) concept to induce BET protein degradation Herein, we present our design, synthesis, and evaluation of a new class of PROTAC BET degraders. One of the most promising compounds, 23, effectively degrades BRD4 protein at concentrations as low as 30 pM in the RS4;11 leukemia cell line, achieves an IC50 value of 51 pM in inhibition of RS4;11 cell growth and induces rapid tumor regression in vivo against RS4;11 xenograft tumors. These data establish that compound 23 (BETd-260/ZBC260) is a highly potent and efficacious BET degrader.

Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Related Products of 82-73-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Huang, Xiubing; Lu, Guilong; Zhang, Kaiyue; Liu, Jijia; Zhang, Hean; Guo, Zhengwei; Tao, Jinzhang published the artcile< Selective synthesis of imines by direct oxidative coupling of amines on Cu-doped CeO2 catalysts>, Application In Synthesis of 3959-07-7, the main research area is imine preparation coupling amine copper doped cerium oxide catalyst.

The study and development of CeO2 nanocrystals containing transition-metal species are of crucial importance for understanding the effect of transition-metal species on their catalytic activity. CeO2 nanocrystals containing only 0.61% Cu were demonstrated as an effective catalyst for imine synthesis from amines at 110° using NHPI as radical initiator and air as oxidant. Especially, Cu-doped CeO2 nanocrystals after thermal treatment at 300° for 2 h show high conversion (97.8%) and high selectivity (98.6%) for the synthesis of N-benzylidene benzylamine from benzylamine, as well as acceptable yield for the synthesis of several other kinds of imines from amines. The Cu-doped CeO2 nanocrystals also exhibited excellent cycling stability for at least four cycles with only a slightly decreased yield. The high catalytic activity of Cu-doped CeO2 can be ascribed to the highly dispersed Cu species and abundant oxygen vacancies on their surfaces which activated the NHPI and O2 and promoted the adsorption/conversion of amine.

Applied Surface Science published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Application In Synthesis of 3959-07-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Li, Han; Sheng, Jie; Wu, Bing-Bing; Li, Yan; Wang, Xi-Sheng published the artcile< Nickel-Catalyzed Cross-Coupling of Ethyl Chlorofluoroacetate with Aryl Bromides>, Synthetic Route of 401-78-5, the main research area is nickel catalyzed cross coupling ethyl chlorofluoroacetate aryl bromide; aryl halides; cross-coupling; ethyl chlorofluoroacetate; monofluoroacetation; nickel.

A combinatorial nickel-catalyzed monofluoroalkylation of aryl bromides with the industrial raw regent Et chlorofluoroacetate has been developed. The two key factors to successful conversion are the combination of nickel with readily available nitrogen and phosphine ligands and the using of a mixture of different solvents. Mechanistic investigations indicated a new zinc regent might generated in situ and be involved in the reaction process.

Chemistry – An Asian Journal published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Synthetic Route of 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cohen, Daniel T.; Cardinal-David, Benoit; Roberts, John M.; Sarjeant, Amy A.; Scheidt, Karl A. published the artcile< NHC-catalyzed/titanium(IV)-mediated highly diastereo- and enantioselective dimerization of enals>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is heterocyclic carbene catalyst titanium diastereoselective enantioselective dimerization enal; unsaturated aldehyde diastereoselective enantioselective dimerization; cyclopentene stereoselective preparation.

An NHC-catalyzed diastereo- and enantioselective dimerization of enals has been developed. The use of Ti(Oi-Pr)4 is a key element for the reactivity and selectivity of this process. The cyclopentenes are obtained with high levels of diastereo- and enantioselectivity and their synthetic utility is demonstrated by functionalization of the product alkene.

Organic Letters published new progress about Carbenes (methylene derivatives) Role: CAT (Catalyst Use), USES (Uses) (heterocyclic carbene). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary