Category: 3893-18-3

Fouque, Amelie; Delalande, Olivier; Jean, Mickael; Castellano, Remy; Josselin, Emmanuelle; Malleter, Marine; Shoji, Kenji F.; Hung, Mac Dinh; Rampanarivo, Hariniaina; Collette, Yves; Weghe, Pierre van de; Legembre, Patrick published the artcile< A Novel Covalent mTOR Inhibitor, DHM25, Shows in Vivo Antitumor Activity against Triple-Negative Breast Cancer Cells>, Electric Literature of 3893-18-3, the main research area is covalent mTOR inhibitor DHM25 antitumor breast cancer.

Constitutive activation of the PI3K/mTOR signaling pathway contributes to carcinogenesis and metastasis in most, if not all, breast cancers. From a chromene backbone reported to inhibit class I PI3K catalytic subunits, several rounds of chem. syntheses led to the generation of a new collection of chromologues that showed enhanced ability to kill PI3K-addicted cancer cells and to inhibit Akt phosphorylation at serine 473, a hallmark of PI3K/mTOR activation. This initial screen uncovered a chromene designated DHM25 that exerted potent antitumor activity against breast tumor cell lines. Strikingly, DHM25 was shown to be a selective and covalent inhibitor of mTOR using biochem. and cellular analyses, modeling, and a large panel of kinase activity assays spanning the human kinome (243 kinases). Finally, in vivo, this novel drug was an efficient inhibitor of growth and metastasis of triple-neg. breast cancer cells, paving the way for its clin. application in oncol.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Electric Literature of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sunden, Henrik; Rios, Ramon; Ibrahem, Ismail; Zhao, Gui-Ling; Eriksson, Lars; Cordova, Armando published the artcile< A highly enantioselective catalytic domino aza-Michael/aldol reaction: one-pot organocatalytic asymmetric synthesis of 1,2-dihydroquinolines>, Application of C9H7BrO, the main research area is stereoselective Michael aldol aminobenzaldehyde unsaturated aldehyde catalyst.

The highly enantioselective organocatalytic domino aza-Michael/aldol reaction is presented. The unprecedented, chiral amine-catalyzed asym. domino reactions between 2-aminobenzaldehydes and α,β-unsaturated aldehydes proceed with excellent chemo- and enantioselectivity to give the corresponding pharmaceutically valuable 1,2-dihydroquinolines in high yields with 90 to > 99 % ee.

Advanced Synthesis & Catalysis published new progress about Aldol condensation catalysts, stereoselective. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Application of C9H7BrO.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yu, Han; Dai, Guoyong; He, Qiu-Rui; Tang, Jiang-Jiang published the artcile< Enantioselective synthesis and evaluation of 4-styryldihydropyrimidin-2-thiones as anti-proliferative agents>, Reference of 3893-18-3, the main research area is styryldihydropyrimidinethione preparation enantioselective anticancer; cinnamaldehyde thiourea ketoester Biginelli reaction organocatalyst.

A series of novel chiral (S)-4-styryldihydropyrimidin-2-thiones I (R1 = H, F, NO2, etc.; R2 = i-Pr, t-Bu; R3 = Me, Et) was prepared with high yields and enantioselective by a Biginelli reaction. In the condensation reaction, substituted cinnamaldehyde R1C6H4CH=CHCHO, thiourea and β-ketoesters R2C(O)CH2C(O)2R3 were organocatalyzed to afford 4-styryldihydropyrimidin-2-thiones I using self-assembled methanoproline-thiourea as catalysts. Anti-proliferative activity of these 4-styryldihydropyrimidin-2-thiones I was tested against the HepG2 and PC-3 cells. Among all the tested compounds, I (R1 = CF3; R2 = i-Pr, t-Bu; R3 = Me, Et) bearing CF3- groups at styryl group displayed a moderate anti-proliferative activity with IC50 ranged between 29.3-38.5 μM. The structure-activity relationship showed that substituents (R1) on the C-4 styryl ring of 4-styryldihydropyrimidin-2-thiones and R3 at ester group affected the anti-proliferative activity, yet R2 at C-6 position had little influence for anti-proliferative activity.

Medicinal Chemistry Research published new progress about Antitumor agents. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Reference of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hong, Bor-Cherng; Lin, Cheng-Wei; Liao, Wei-Kai; Lee, Gene-Hsiang published the artcile< Sequential Asymmetric Catalysis in Michael-Michael-Michael-Aldol Reactions: Merging Organocatalysis with Photoredox Catalysis in a One-Pot Enantioselective Synthesis of Highly Functionalized Decalines Bearing a Quaternary Carbon Stereocenter>, HPLC of Formula: 3893-18-3, the main research area is enantioselective synthesis decalin Michael Michael aldol organocatalyst photochem.

An expedited method has been developed for the enantioselective synthesis of highly functionalized decaline systems (e.g., I) containing seven contiguous stereogenic centers with high enantioselectivities (>99% ee). The one-pot methodol. comprises a cascade of organocatalytic double Michael-photocatalyzed Michael-aldol reactions of Et 2-bromo-6-formylhex-2-enoate, β-alkyl-α,β-unsaturated aldehydes, and α-alkyl-α,β-unsaturated aldehydes. The structure and absolute configuration of an appropriate product were confirmed by X-ray anal.

Organic Letters published new progress about Aldol addition. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, HPLC of Formula: 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Meazza, Marta; Leth, Lars A.; Erickson, Jeremy D.; Jorgensen, Karl Anker published the artcile< Indium(III)-catalyzed Aza-Conia-Ene Reaction for the Synthesis of Indolizines>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is indolizine pyrroloquinoline preparation aza Conia ene cyclization indium catalyst; heterocycles; indium; indolizines; synergistic catalysis.

A new indium(III)-catalyzed reaction for the synthesis of a series of indolizine scaffolds has been developed. This methodol. was highly efficient, allowing a low catalyst loading of 2 mol % (down to 0.5 mol %) and rendering the products in high yields through a 5-exo-dig aza-Conia-ene reaction. Furthermore, the possibility of incorporating an electrophile into the generated pyrrolidone ring in a one-pot synergistic fashion was demonstrated. Finally, based on exptl. observations, a mechanism proposal was outlined.

Chemistry – A European Journal published new progress about Enantioselective synthesis. 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

Feng, Xin; Cui, Hai-Lei; Xu, Shi; Wu, Li; Chen, Ying-Chun published the artcile< Organocatalytic Direct Vinylogous Michael Addition of α,β-Unsaturated γ-Butyrolactam to α,β-Unsaturated Aldehydes and an Illustration to Scaffold Diversity Synthesis>, Formula: C9H7BrO, the main research area is alkyl butyrolactam stereoselective preparation; unsaturated butyrolactam aldehyde diastereoselective enantioselective regioselective chemoselective Michael addition; alkaloid stereoselective preparation; butyrolactam reductive amination intramol aza Michael addition; diastereoselective reductive radical conjugate addition cyclization.

The first organocatalytic regio- and chemoselective direct vinylogous Michael addition of N-Boc α,β-unsaturated γ-butyrolactam to α,β-unsaturated aldehydes is reported. The desired adducts, e.g. I, with multiple orthogonal sets of functionalities were obtained in excellent enantioselectivity (up to 98% ee) with low to outstanding diastereoselectivity (d.r. up to > 20:1). Moreover, it has been demonstrated that the products were quite valuable for scaffold diversity synthesis. A number of enantioenriched natural-product-like or drug-like mols. with fused bi-, tri-, and polycyclic structures, e.g. II, have been efficiently constructed, which might have potentials in the later explorations for the biol. related studies.

Chemistry – A European Journal published new progress about Alkaloids Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Formula: C9H7BrO.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Barik, Soumen; Das, Rohan Chandra; Balanna, Kuruva; Biju, Akkattu T. published the artcile< Kinetic Resolution Approach to the Synthesis of C-N Axially Chiral N-Aryl Aminomaleimides via NHC-Catalyzed [3 + 3] Annulation>, Category: bromides-buliding-blocks, the main research area is phenyl aminopyrrolidione bromopropenal arene heterocyclic carbene cycloaddition kinetic resolution; aryl pyrrolopyridine trione preparation.

Chiral NHC-catalyzed kinetic resolution of N-aryl aminomaleimides allowing the synthesis of C-N axially chiral N-aryl aminomaleimides via remote chirality control was presented. The catalytically generated α,β-unsaturated acylazoliums from 2-bromoenals underwent selective [3 + 3] annulation with one of the enantiomers of maleimide to furnish fused-dihydropyridinone (bearing axial/central chirality, up to 6:1 dr, >99:1 er) leaving the enantioenriched opposite enantiomer (up to >99:1 er). Studies on C-N bond rotation barrier and dependence on temperature were also provided.

Organic Letters published new progress about [3+3] Cycloaddition reaction (stereoselective). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chen, Xiang-Yu; Chen, Kun-Quan; Sun, De-Qun; Ye, Song published the artcile< N-Heterocyclic carbene-catalyzed oxidative [3+2] annulation of dioxindoles and enals: cross coupling of homoenolate and enolate>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is spirocyclic oxindole lactone preparation; dioxindole enal oxidative annulation heterocyclic carbene catalyst.

The N-heterocyclic carbene-catalyzed oxidative [3+2] annulation of dioxindoles I (R = H, Bn; X = H, 4-Br, 5-H3CO, 6-Br) and enals R1CH=CHCHO (R1 = n-C6H13, HC=CHCH3, 4-FC6H4, etc.) was developed for giving the corresponding spirocyclic oxindole-γ-lactones II and III in good yields with high to excellent diastereo- and enantioselectivities. The challenging aliphatic enals worked effectively using this strategy. The oxidative cross coupling of homoenolate and enolate via single electron transfer was proposed as the key step for the reaction.

Chemical Science published new progress about Cross-coupling reaction, stereoselective. 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

Zheng, Pengcheng; Li, Chengcheng; Mou, Chengli; Pan, Dingwu; Wu, Shuquan; Xue, Wei; Jin, Zhichao; Chi, Yonggui Robin published the artcile< Efficient Access to 2-Pyrones via Carbene-Catalyzed Oxidative [3+3] Reactions between Enals and Nitrogen Ylides>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is pyrone preparation; enal nitrogen ylide oxidative cycloaddition carbene catalyst.

A carbene-catalyzed oxidative [3+3] cycloaddition reaction between enals and nitrogen ylides for quick access to 2-pyrones I [R = Et, Ph, 2-naphthyl, etc.; Ar = Ph, 4-BrC6H4, 2-furyl, etc.] was reported. Inexpensive and easily prepared 2′-pyridinium bromide salts were used as precursors of pyridinium ylides to react with enals in this catalytic reactions.

Asian Journal of Organic Chemistry published new progress about [3+3] Cycloaddition reaction. 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

Ressmann, Anna K.; Schwendenwein, Daniel; Leonhartsberger, Simon; Mihovilovic, Marko D.; Bornscheuer, Uwe T.; Winkler, Margit; Rudroff, Florian published the artcile< Substrate-Independent High-Throughput Assay for the Quantification of Aldehydes>, Product Details of C9H7BrO, the main research area is aldehyde quantification high throughput assay aminobenzamidoxime derivative.

The selective and direct reduction of carboxylic acids into the corresponding aldehydes by chem. methods is still a challenging task in synthesis. Several reductive and oxidative chem. methods are known to produce aldehydes, but most of them require expensive reagents, special reaction conditions, are 2-step procedures and often lack chemoselectivity. Nature provides an elegant tool, so called carboxylic acid reductases (CARs) for the direct reduction of carboxylic acids to aldehydes. Discovery as well as engineering of novel CAR enzymes necessitates a robust, product selective high-throughput assay (HTA). The authors report a simple and fast HTA that allows the substrate-independent and chemoselective quantification of aldehydes (irresp. of their chem. structure) and is sensitive to the nM range. The HTA was validated by NMR and GC analyses and in microbial cells by reexamination of the substrate scope of CAR from Nocardia iowensis (CARNi). The results were fully consistent with reported data.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: ANT (Analyte), RCT (Reactant), SPN (Synthetic Preparation), ANST (Analytical Study), RACT (Reactant or Reagent), PREP (Preparation). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Product Details of C9H7BrO.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary