Month: October 2022

Wang, Huamin; Cai, Jinhui; Huang, Huawen; Deng, Guo-Jun published the artcile< Palladium-Catalyzed Phthalazinone Synthesis Using Paraformaldehyde as Carbon Source>, Product Details of C8H6BrFO2, the main research area is methyl benzoate paraformaldehyde aryl hydrazine cyclocondensation palladium catalyst; phthalazinone preparation.

A palladium-catalyzed one-pot synthesis of phthalazinones I [ Ar = ph, 4-Me-ph, 4-Et-ph, 4-OMe-ph, etc.] from 2-halomethyl benzoates, paraformaldehyde, and aryl hydrazines is described. Various substituted phthalazinones were selectively obtained in good yields using paraformaldehyde as the cheap carbon source (CH).

Organic Letters published new progress about Addition reaction catalysts. 6942-39-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H6BrFO2, Product Details of C8H6BrFO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhao, Liang-Liang; Li, Xing-Shuo; Cao, Li-Li; Zhang, Rui; Shi, Xiao-Qian; Qi, Jing published the artcile< Access to dihydropyridinones and spirooxindoles: application of N-heterocyclic carbene-catalyzed [3+3] annulation of enals and oxindole-derived enals with 2-aminoacrylates>, HPLC of Formula: 3893-18-3, the main research area is dihydropyridinone preparation; spirooxindole preparation; enal aminoacrylate annulation heterocyclic carbene catalyst.

A strategy for the NHC-catalyzed synthesis of dihydropyridinones I (R = C6H5HC=CH, C6H5, 3-thienyl, et.; R1 = Me, Et), II and spirooxindoles III (R2 = Me, allyl, benzyl; R3 = Me, Et; R4 = H, 5-Me, 6-Br, etc.) has been developed via [3+3] annulation reactions of enals RHC=CHCHO or isatin-derived enals IV with 2-aminoacrylates TsNHC(=CH2)C(O)2R1 under oxidative conditions. In this efficient strategy, the 2-aminoacrylates served as nucleophiles. Modifying the standard base switched the carbon-carbon double bond formation from 5,6-positions to 3,4-positions to generate 5,6-dihydropyridinones I and 3,4-dihydropyridinones II, resp. Meanwhile, a diverse set of spirooxindole derivatives was also synthesized in good to excellent yields.

Chemical Communications (Cambridge, United Kingdom) published new progress about Cyclization. 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

Rueping, Magnus; Dufour, Jeremy; Maji, Modhu Sudan published the artcile< Relay catalysis: combined metal catalyzed oxidation and asymmetric iminium catalysis for the synthesis of bi- and tricyclic chromenes>, Quality Control of 3893-18-3, the main research area is chiral bicyclic tricyclic chromene preparation; asym oxidative iminium allenamine cascade propargyl alc.

A catalytic asym. oxidative iminium-allenamine cascade allows the use of propargyl alcs. as stable substrates and yields valuable chiral bicyclic 4H-chromenes. E.g., in presence of prolinol derivative (I), tetrapropylammonium perruthenate, and N-methylmorpholine N-oxide, the enantioselective oxidative cascade of (E)-HOC6H4CH:CHNO2 and PhCCCH2OH gave 81% chiral bicyclic 4H-chromene (II). A subsequent Michael addition-condensation domino reaction provides complex tricyclic 4H-chromenes in a highly enantioselective fashion.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alcohols, propargyl Role: RCT (Reactant), RACT (Reactant or Reagent). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Quality Control of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Eckert, Timothy; Harmeyer, Grace; Legate, Steven; Mathe, Steven published the artcile< A Rationale for the Ortho Effect in Electrophilic Aromatic Substitutions>, COA of Formula: C7H4BrF3, the main research area is electrophilic aromatic substitution ortho effect.

The ortho effect arises in certain electrophilic aromatic substitutions when a meta director is meta to an ortho/para director. Among the three expected isomer products, only the two isomers ortho to the meta director were produced normally. To find an explanation for the ortho effect, nitrations of two properly substituted benzenes were explored. Evidence supported an explanation based on resonance involving the meta director.

Letters in Organic Chemistry published new progress about Electrophilic aromatic substitution reaction. 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, COA of Formula: C7H4BrF3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Gotoh, Hiroaki; Ishikawa, Hayato; Hayashi, Yujiro published the artcile< Diphenylprolinol Silyl Ether as Catalyst of an Asymmetric, Catalytic, and Direct Michael Reaction of Nitroalkanes with α,β-Unsaturated Aldehydes>, SDS of cas: 3893-18-3, the main research area is silyl ether stereoselective Michael addition catalyst nitroalkane unsaturated aldehyde.

A catalytic enantioselective direct conjugate addition of nitroalkanes to α,β-unsaturated aldehydes using diphenylprolinol silyl ether as an organic catalyst has been developed. Using this methodol. as a key step, short syntheses of therapeutically useful compounds have also been accomplished. For example, the reaction of 4-chlorocinnamaldehyde with nitromethane using (2S)-2-[diphenyl[(trimethylsilyl)oxy]methyl]pyrrolidine as catalyst gave (-)-(βS)-4-chloro-β-(nitromethyl)benzenepropanal. The latter was converted into (βS)-4-chloro-β-(nitromethyl)benzenepropanoic acid, which is a precursor for (S)-baclofen.

Organic Letters published new progress about Aldehydes Role: SPN (Synthetic Preparation), PREP (Preparation) (nitro). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, SDS of cas: 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wu, Ping; Qu, Jinpeng; Li, Yaxuan; Guo, Xin; Tang, Dong; Meng, Xu; Yan, Rulong; Chen, Baohua published the artcile< Iron(III)/Iodine-Catalyzed C(sp2)-H Activation of α,β-Unsaturated Aldehydes/Ketones with Amidines: Synthesis of 1,2,4,5-Tetrasubstituted Imidazoles>, Quality Control of 3893-18-3, the main research area is tetrasubstituted imidazole preparation; enone enal amidine heterocyclization iron iodine catalyst.

An efficient methodol. to access a library of 1,2,4,5-tetrasubstituted imidazoles from a broad range of amidines and α,β-unsaturated aldehydes/ketones via a C(sp2)-H amination has been developed. This method represents a new and simple way to prepare highly substituted imidazoles from easily available starting materials, inexpensive catalysts, and with good functional group tolerance in good to excellent yields.

Advanced Synthesis & Catalysis published new progress about Amidines Role: RCT (Reactant), RACT (Reactant or Reagent). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Quality Control of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Kim, Ji Hye; Constantin, Timothee; Simonetti, Marco; Llaveria, Josep; Sheikh, Nadeem S.; Leonori, Daniele published the artcile< A radical approach for the selective C-H borylation of azines>, HPLC of Formula: 401-78-5, the main research area is borylation azine radical addition approach aminborane reagent; radical addition free energy azine borylation; crystal structure borylated azine boraneylmethylquinoline trimethylamine complex; mol structure borylated azine boraneylmethylquinoline trimethylamine complex.

B functional groups are often introduced in place of aromatic C-H bonds to expedite small-mol. diversification through coupling of mol. fragments1-3. Current approaches based on transition-metal-catalyzed activation of C-H bonds are effective for the borylation of many (hetero)aromatic derivatives4,5 but show narrow applicability to azines (N-containing aromatic heterocycles), which are key components of many pharmaceutical and agrochem. products6. Here the authors report an azine borylation strategy using stable and inexpensive amine-borane7 reagents. Photocatalysis converts these low-mol.-weight materials into highly reactive boryl radicals8 that undergo efficient addition to azine building blocks. This reactivity provides a mechanistically alternative tactic for sp2 C-B bond assembly, where the elementary steps of transition-metal-mediated C-H bond activation and reductive elimination from azine-organometallic intermediates are replaced by a direct, Minisci9-style, radical addition The strongly nucleophilic character of the amine-boryl radicals enables predictable and site-selective C-B bond formation by targeting the azine’s most activated position, including the challenging sites adjacent to the basic N atom. This approach enables access to aromatic sites that elude current strategies based on C-H bond activation, and led to borylated materials that would otherwise be difficult to prepare The authors have applied this process to the introduction of amine-borane functionalities to complex and industrially relevant products. The diversification of the borylated azine products by mainstream cross-coupling technologies establishes aromatic amino-boranes as a powerful class of building blocks for chem. synthesis.

Nature (London, United Kingdom) published new progress about Addition reaction catalysts (tetra(carbazolyl)dicyanobenzene). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, HPLC of Formula: 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Mayer, Nicole; Schweiger, Martina; Fuchs, Elisabeth; Migglautsch, Anna K.; Doler, Carina; Grabner, Gernot F.; Romauch, Matthias; Melcher, Michaela-Christina; Zechner, Rudolf; Zimmermann, Robert; Breinbauer, Rolf published the artcile< Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL)>, Application In Synthesis of 5751-83-7, the main research area is PNPLA2 lipolysis NAFLD atglistatin murine ATGL inhibitors SAR; Atglistatin; Lipolysis; NAFLD; PNPLA2; Small molecule inhibitor.

High serum fatty acid (FA) levels are causally linked to the development of insulin resistance, which eventually progresses to type 2 diabetes and non-alc. fatty liver disease (NAFLD) generalized in the term metabolic syndrome. Adipose triglyceride lipase (ATGL) is the initial enzyme in the hydrolysis of intracellular triacylglycerol (TG) stores, liberating fatty acids that are released from adipocytes into the circulation. Hence, ATGL-specific inhibitors have the potential to lower circulating FA concentrations, and counteract the development of insulin resistance and NAFLD. In this article, we report about structure-activity relationship (SAR) studies of small mol. inhibitors of murine ATGL which led to the development of Atglistatin. Atglistatin is a specific inhibitor of murine ATGL, which has proven useful for the validation of ATGL as a potential drug target.

Bioorganic & Medicinal Chemistry published new progress about Drug targets. 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Application In Synthesis of 5751-83-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Poornima, B.; Venkanna, A.; Swetha, B.; Kamireddy, Karthik Reddy; Siva, Bandi; Phani Babu, V. S.; Ummanni, Ramesh; Babu, K. Suresh published the artcile< Total synthesis, biological evaluation of dendrodolides A-D and their analogues>, Quality Control of 16426-64-5, the main research area is dendrodolide synthesis anticancer.

A concise total synthesis of dendrodolides A-D has been accomplished in 10 steps from com. available (R)-propylene oxide and 3-buten-1-ol as starting materials. The key steps involved in the synthesis are Jacobsen hydrolytic kinetic resolution, epoxide ring opening with 2-allyl-1,3-dithiane, Yamaguchi esterification and ring-closing metathesis (RCM). In addition, a series of ester derivatives were prepared utilizing Yamaguchi esterification at the C-3 position of the dendrodolide core and screened for their efficacy against cancer cell lines.

Tetrahedron published new progress about Antitumor agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Quality Control of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Dvorakova, Marcela; Langhansova, Lenka; Temml, Veronika; Pavicic, Antonio; Vanek, Tomas; Landa, Premysl published the artcile< Synthesis, Inhibitory Activity and In Silico Modeling of Selective COX-1 Inhibitors with a Quinazoline Core>, Application In Synthesis of 20776-50-5, the main research area is quinazoline preparation cyclooxygenase inhibitor docking.

Three series of quinazoline derivatives I [R1 = 4-H2NC6H4O, 4-MeOC6H4CH2NH, 4-MeC6H4NH, etc.; R2 = CH:CHPh, Et2N, morpholino, pyrrolidin-1-yl, piperazin-1-yl; R3 = H, 4-MeOC6H4, 4-FC6H4, 2-thienyl] were prepared and tested for their potential inhibitory activity toward COX-1 and COX-2. Of the prepared compounds, 11 exhibited interesting COX-1 selectivity, with 8 compounds being totally COX-1-selective. The IC50 value of the best quinazoline inhibitor was 64 nM. The structural features ensuring COX-1 selectivity were elucidated using in silico modeling.

ACS Medicinal Chemistry Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Application In Synthesis of 20776-50-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary