Category: 112253-70-0

Li, Feng; Lu, Lei; Liu, Pengcheng published the artcile< Acceptorless Dehydrogenative Coupling of o-Aminobenzamides with the Activation of Methanol as a C1 Source for the Construction of Quinazolinones>, Electric Literature of 112253-70-0, the main research area is dehydrogenative coupling aminobenzamide methanol iridium catalyst; quinazolinone preparation dehydrogenative coupling aminobenzamide methanol iridium catalyst.

A strategy for the synthesis of quinazolinones I (R = H, 7-Me, 6-MeO, 8-F, etc.) via acceptorless coupling of o-aminobenzamides with methanol has been accomplished in the presence of the metal-ligand bifunctional catalyst [Cp*Ir(2,2′-bpyO)(H2O)]. Notably, this research exhibited the potential of transition-metal-catalyzed activation of methanol as a C1 source for the construction of heterocycles.

Organic Letters published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (o-aminobenzamides). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Electric Literature of 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kwiatkowski, Jacek; Liu, Boping; Pang, Shermaine; Binte Ahmad, Nur Huda; Wang, Gang; Poulsen, Anders; Yang, Haiyan; Poh, Yong Rui; Tee, Doris Hui Ying; Ong, Esther; Retna, Priya; Dinie, Nurul; Kwek, Perlyn; Wee, John Liang Kuan; Manoharan, Vithya; Low, Choon Bing; Seah, Peck Gee; Pendharkar, Vishal; Sangthongpitag, Kanda; Joy, Joma; Baburajendran, Nithya; Jansson, Anna Elisabet; Nacro, Kassoum; Hill, Jeffrey; Keller, Thomas H.; Hung, Alvin W. published the artcile< Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2>, Name: 2-Amino-4-bromobenzamide, the main research area is pyridine benzamide preparation mitogen protein kinase pharmacokinetic SAR docking.

Dysregulation of translation initiation factor 4E (eIF4E) activity occurs in various cancers. Mitogen-activated protein kinase (MAPK) interacting kinases 1 and 2 (MNK1 and MNK2) play a fundamental role in activation of eIF4E. Structure-activity relationship-driven expansion of a fragment hit led to discovery of dual MNK1 and MNK2 inhibitors based on a novel pyridine-benzamide scaffold. The compounds possess promising in vitro and in vivo pharmacokinetic profiles and show potent on target inhibition of eIF4E phosphorylation in cells.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Name: 2-Amino-4-bromobenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Liu, Wei; Wu, Ge; Gao, Wenxia; Ding, Jinchang; Huang, Xiaobo; Liu, Miaochang; Wu, Huayue published the artcile< Palladium-catalyzed oxidative C=C bond cleavage with molecular oxygen: one-pot synthesis of quinazolinones from 2-amino benzamides and alkenes>, Recommanded Product: 2-Amino-4-bromobenzamide, the main research area is aminobenzamide alkene palladium catalyst one pot tandem reaction; arylquinazolinone preparation green chem.

Palladium-catalyzed oxidative cleavage/cyclization was disclosed for the concise synthesis of various quinazolinone derivatives from readily available 2-aminobenzamides and terminal alkenes with excellent functional group tolerance. The synthetic features regarding the use of oxygen as a green oxidant and its utility were illustrated in the synthesis of sildenafil.

Organic Chemistry Frontiers published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Recommanded Product: 2-Amino-4-bromobenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kerdphon, Sutthichat; Jongcharoenkamol, Jira; Chatwichien, Jaruwan; Singh, Thishana; Channei, Duangdao; Choommongkol, Vachira; Rithchumpon, Puracheth; Meepowpan, Puttinan published the artcile< Microwave-Assisted Green Synthesis of 2,3-Dihydroquinazolinones under Base- and Catalyst-Free conditions>, COA of Formula: C7H7BrN2O, the main research area is dihydroquinazolinone acetonitrile cinnamaldehyde aldehyde butyraldehyde irradiation hydrolysis.

A facile and green one-pot synthesis of 2,3-dihydroquinazolinones, using microwave irradiation, has been developed. Dihydroquinazolinones were synthesized from 2-aminobenzamide derivatives and various aldehydes in aqueous solution under base and catalyst free reaction conditions. The desired products, from aliphatic and aromatic aldehydes substrates, were obtained in 5 min with up to 99 % isolated yields.

ChemistrySelect published new progress about Aldehydes Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, COA of Formula: C7H7BrN2O.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Guo, Yongbiao; Gao, Zhenhua; Li, Junchen; Bi, Xiaojing; Shi, Enxue; Xiao, Junhua published the artcile< Practical catalytic enantioselective synthesis of 2,3-dihydroquin-azolinones by chiral bronsted acid catalysis>, Name: 2-Amino-4-bromobenzamide, the main research area is dihydroquinazolinone preparation enantioselective.

Herein, The highly efficient and practical synthesis of 2,3-dihydroquinazolinones I [R1 = n-Pr, cyclohexyl, Ph, etc.; R2 = H, Me, allyl; R3 = H, Me; R4 = H, 6-Me, 7-Cl, etc.; X = O, S] directly from diverse aldehydes with excellent yields and enantioselectivity was reported. Particularly, this protocol afforded better enantiocontrol for aliphatic aldehydes (up to 99% yield, 97% ee), which always gave unsatisfactory results in the previous studies. Moreover, this catalytic system showed wide tolerance to different functional groups such as alkenyl, nitro and halogens. Most importantly, its practicability was well elucidated via the gram-scale synthesis of different types of products at 0.1 mol% catalyst loading and the simplified work-up procedure. To better understand the reaction pathway and origin of the enantioselectivity, DFT calculations were also performed.

Organic & Biomolecular Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Name: 2-Amino-4-bromobenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Talamas, Francisco X.; Abbot, Sarah C.; Anand, Shalini; Brameld, Ken A.; Carter, David S.; Chen, Jun; Davis, Dana; de Vicente, Javier; Fung, Amy D.; Gong, Leyi; Harris, Seth F.; Inbar, Petra; Labadie, Sharada S.; Lee, Eun K.; Lemoine, Remy; Le Pogam, Sophie; Leveque, Vincent; Li, Jim; McIntosh, Joel; Najera, Isabel; Park, Jaehyeon; Railkar, Aruna; Rajyaguru, Sonal; Sangi, Michael; Schoenfeld, Ryan C.; Staben, Leanna R.; Tan, Yunchou; Taygerly, Joshua P.; Villasenor, Armando G.; Weller, Paul E. published the artcile< Discovery of N [4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]-methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase>, Application In Synthesis of 112253-70-0, the main research area is oxopyridinyl butylquinolinylphenyl methanesulfonamide preparation hepatitis C virus polymerase inhibitor.

In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we discuss our efforts that led to the identification of a bicyclic template with potent activity against the NS5B polymerase, a critical enzyme on the life cycle of HCV. In continuation of our exploration to improve the stilbene series, the 3,5,6,8-tetrasubstituted quinoline core was identified as replacement of the stilbene moiety. 6-Methoxy-2-(1H)-pyridone was identified among several heterocyclic headgroups to have the best potency. Solubility of the template was improved by replacing a planar aryl linker with a saturated pyrrolidine. Profiling of the most promising compounds led to the identification of quinoline I (RG7109), which was selected for advancement to clin. development.

Journal of Medicinal Chemistry published new progress about Antiviral agents (hepatitis C). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Application In Synthesis of 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Narasimhamurthy, Kereyagalahally H.; Chandrappa, Siddappa; Sharath Kumar, Kothanahally S.; Harsha, Kachigere B.; Ananda, Hanumappa; Rangappa, Kanchugarakoppal S. published the artcile< Easy access for the synthesis of 2-aryl 2,3-dihydroquinazolin-4(1H)-ones using gem-dibromomethylarenes as synthetic aldehyde equivalent>, Computed Properties of 112253-70-0, the main research area is quinazolinone dihydro aryl preparation.

One step synthesis of 2,3-dihydroquinazolin-4(1H)-ones I (R = H, Cl, OCH3; R1 = H, Br, Cl, OCH3; Ar = 3-ClC6H4, 4-pyridyl, 4-CF3C6H4, etc.) from gem-dibromomethylarenes ArCH(Br)2 using 2-aminobenzamide is described. Gem-dibromomethylarenes are used as aldehyde equivalent for the efficient synthesis of 2,3-dihydroquinazolin-4(1H)-ones, this synthesis takes shorter reaction time with quick isolation and excellent product yield.

RSC Advances published new progress about Amino amides Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Computed Properties of 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Joshi, Vidya; Chaudhari, Rajendra P. published the artcile< Synthesis of some new 4-quinazolinone-2-carboxylic acid esters, -2-carboxamides, -2-carbohydrazides and their tosyl derivatives having potential biological activity>, Formula: C7H7BrN2O, the main research area is quinazolinecarbohydrazide preparation antitubercular.

Quinazolinecarbohydrazides I [R1 = H, Me, OMe, halo, and R2 = H; R1R2 = (CH2O2)] were prepared from the resp. anthranilamides by cyclocondensation with EtO2CCO2Et and subsequent amidation with N2H4; I showed antitubercular activity. Also prepared were tosyl derivatives II.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Tuberculostatics. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Formula: C7H7BrN2O.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Kikelj, D. published the artcile< Product class 13: quinazolines>, Electric Literature of 112253-70-0, the main research area is review quinazoline preparation; ring closure transformation quinazoline preparation review; aromatization quinazoline preparation review; substituent modification quinazoline preparation review.

A review. Preparation of quinazolines by ring closure and ring transformation reactions as well as aromatization and substituent modification is given.

Science of Synthesis published new progress about 112253-70-0. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Electric Literature of 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Liu, Zhiqing; Chen, Haiying; Wang, Pingyuan; Li, Yi; Wold, Eric A.; Leonard, Paul G.; Joseph, Sarah; Brasier, Allan R.; Tian, Bing; Zhou, Jia published the artcile< Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation>, SDS of cas: 112253-70-0, the main research area is arylquinazolinone arylchromone preparation inhibitor BRD4 antiinflammatory agent; structure arylquinazolinone arylchromone antiinflammatory activity inhibition BRD4; selectivity arylchromone inhibition BRD4 pharmacokinetics metabolism hERG CYP.

Arylquinazolinones and arylchromenones such as I (X = CH2, MeN) were prepared as selective inhibitors of bromodomain-containing protein 4 (BRD4) for potential use as orally bioavailable antiinflammatory agents. I inhibited BRD4 with IC50 values of 67-84 nM and were selective for BRD1 over binding domains of BRD2, BRD3, and BRDT and over CBP; I inhibited the expression of Toll-like receptor (TLR3)-induced inflammatory genes in vitro and inhibited airway inflammation in mice. The pharmacokinetics (t1/2, AUC, Cmax, and clearance), metabolic stability of I (X = NMe) in murine and human cells, and inhibition of cytochrome P450 enzymes and hERG by I (X = MeN) were determined The structure of I (X = NMe) bound to human BRD4 binding domain 1 was determined by X-ray crystallog.

Journal of Medicinal Chemistry published new progress about Anti-inflammatory agents. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, SDS of cas: 112253-70-0.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics