Month: October 2022

Bezencon, Olivier; Bur, Daniel; Weller, Thomas; Richard-Bildstein, Sylvia; Remen, Lubos; Sifferlen, Thierry; Corminboeuf, Olivier; Grisostomi, Corinna; Boss, Christoph; Prade, Lars; Delahaye, Stephane; Treiber, Alexander; Strickner, Panja; Binkert, Christoph; Hess, Patrick; Steiner, Beat; Fischli, Walter published the artcile< Design and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors>, SDS of cas: 56724-03-9, the main research area is aryl substituted diazabicyclononenecarboxamide preparation selective renin inhibitor antihypertensive; potent nonpeptidic bioavailable diazabicyclononenecarboxamide renin inhibitor; structure aryl substituted diazabicyclononenecarboxamide inhibition renin; mol crystal structure renin bound nonracemic aryloxyethylphenyl diazabicyclononenecarboxamide.

Aryl-substituted diazabicyclononenecarboxamides such as I are prepared as selective human renin inhibitors for potential use as antihypertensive agents. Aryl substituents and the carboxamide moiety of the diazabicyclononenecarboxamides are essential for selective binding to renin; attachment of a substituent to the methyleneaminomethylene bridge of the diazabicyclononenecarboxamides does not modify the binding affinity but alters the pharmacokinetics of the product. I inhibits renin with an IC50 of 0.20 nM in buffer and 19 nM in plasma; a 10 mg/kg dose of I lowers the blood pressures of transgenic rats over a period of 36 h. The structures of both enantiomers of an aryloxyethylphenyl diazabicyclononenecarboxamide sep. bound to human renin are determined by X-ray crystallog.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 56724-03-9 belongs to class ethers-buliding-blocks, and the molecular formula is C9H10O2, SDS of cas: 56724-03-9.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Gevorgyan, Ashot; Hopmann, Kathrin H.; Bayer, Annette published the artcile< Formal C-H Carboxylation of Unactivated Arenes>, Recommanded Product: 2-(2-Methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, the main research area is carboxyl unactivated arene preparation green chem regioselective; unactivated arene carbon dioxide carboxylation copper catalyst; carbon dioxide aryl boronate carboxylation copper catalyst; C−H activation; carbon dioxide; carboxylation; green solvent; late-stage functionalization.

A formal C-H carboxylation of unactivated arenes e.g., I using CO2 in green solvents is described. The present strategy combines a sterically controlled Ir-catalyzed C-H borylation followed by a Cu-catalyzed carboxylation of the in situ generated organoboronates. The reaction is highly regioselective for the C-H carboxylation of unactivated arenes e.g., I (1,3-disubstituted and 1,2,3-trisubstituted benzenes, 1,2- or 1,4-sym. substituted benzenes, fluorinated benzenes and different heterocycles). The developed methodol. was applied to the late-stage C-H carboxylation of com. drugs and ligands.

Chemistry – A European Journal published new progress about Aromatic carboxylic acids Role: SPN (Synthetic Preparation), PREP (Preparation). 190788-60-4 belongs to class ethers-buliding-blocks, and the molecular formula is C13H19BO3, Recommanded Product: 2-(2-Methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Popa, Adriana; Davidescu, Corneliu-Mircea; Trif, Radu; Ilia, Gheorghe; Iliescu, Smaranda; Dehelean, Gheorghe published the artcile< Polycationic biocides with pendant quaternary groups. II. Synthesis and antimicrobial activity of ammonium salts grafted on ""gel""-type styrene-divinylbenzene copolymers against Staphylococcus aureus and escherichia coli>, Safety of 2,2′-(Tridecylazanediyl)diethanol, the main research area is quaternary chloromethylated styrene divinylbenzene copolymer antimicrobial agent.

Various ammonium salts grafted on “”gel””-type styrene-divinylbenzene copolymers were prepared and their antimicrobial activity against Staphylococcus aureus and Escherichia coli was assessed by the column system. The antimicrobial activity is strongly dependent on the structure. The length of the alkyl chain has been found to affect significantly the biol. activity.

Revue Roumaine de Chimie published new progress about Antimicrobial agents. 18312-57-7 belongs to class ethers-buliding-blocks, and the molecular formula is C17H37NO2, Safety of 2,2′-(Tridecylazanediyl)diethanol.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Gilmartin, Philip H.; Kozlowski, Marisa C. published the artcile< Vanadium-Catalyzed Oxidative Intramolecular Coupling of Tethered Phenols: Formation of Phenol-Dienone Products>, HPLC of Formula: 56724-03-9, the main research area is vanadium catalyzed oxidative intramol coupling tethered phenol dienone.

A mild and efficient method for the vanadium-catalyzed intramol. coupling of tethered free phenols is described. The corresponding phenol-dienone products are prepared directly in good yields with low catalyst loadings. Electronically diverse tethered phenol precursors are well tolerated, and the catalytic method was effectively applied as the key step in syntheses of three natural products and a synthetically useful morphinan alkaloid precursor.

Organic Letters published new progress about Biomimetic synthesis. 56724-03-9 belongs to class ethers-buliding-blocks, and the molecular formula is C9H10O2, HPLC of Formula: 56724-03-9.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Ding, Decai; Dong, Haiyan; Wang, Chuan published the artcile< Nickel-Catalyzed Asymmetric Domino Ring Opening/Cross-Coupling Reaction of Cyclobutanones via a Reductive Strategy>, Quality Control of 6482-24-2, the main research area is chiral indanone preparation enantioselective; cyclobutanone alkylbromide ring opening tandem coupling reduction nickel catalyst; Catalysis; Organic Reaction; Organic Synthesis.

The successful application of reductive strategy in the asym. domino ring opening/cross-coupling reaction of prochiral cyclobutanones I (R = Me, Et, n-Pr; R1 = H, Me, F, etc.; R2 = H, Me, OCH3) was demonstrated. Under the catalysis of a chiral nickel complex, various aryl iodide-tethered cyclobutanones I were reacted with alkyl bromides R3Br (R3 = 2-methoxyethyl, cyclopentyl, oxan-4-yl, etc.) as the electrophilic coupling partner, providing a variety of chiral indanones II bearing a quaternary stereogenic center in highly enantioselective manner, which can be further converted to diverse benzene-fused cyclic compounds including III, IV, V (X = O, NH). The preliminary mechanistic investigations support a mechanism involving Ni(I)-mediated enantiotopic C-C σ-bond activation of cyclobutanones as key elementary step in the catalytic cycle.

iScience published new progress about Bond activation catalysts (C-C). 6482-24-2 belongs to class ethers-buliding-blocks, and the molecular formula is C3H7BrO, Quality Control of 6482-24-2.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Ochiai, Koji; Takita, Satoshi; Eiraku, Tomohiko; Kojima, Akihiko; Iwase, Kazuhiko; Kishi, Tetsuya; Fukuchi, Kazunori; Yasue, Tokutaro; Adams, David R.; Allcock, Robert W.; Jiang, Zhong; Kohno, Yasushi published the artcile< Phosphodiesterase inhibitors. Part 3: Design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-dihydropyridazinones with anti-inflammatory and bronchodilatory activity>, Recommanded Product: 2-Amino-3-methoxyphenol, the main research area is pyridazinone dihydro heteroaromatic preparation antiinflammatory bronchodilatory activity.

(-)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. A survey of potential bicyclic heteroaromatic replacement subunits for the pyrazolo[1,5-a]pyridine core of KCA-1490 has identified the 4-methoxy-2-(trifluoromethyl)benzo[d]thiazol-7-yl and 8-methoxy-2-(trifluoromethyl)quinolin-5-yl analogs as dual PDE3/4-inhibitory compounds that potently suppress histamine-induced bronchoconstriction and exhibit anti-inflammatory activity in vivo.

Bioorganic & Medicinal Chemistry published new progress about Anti-inflammatory agents. 40925-69-7 belongs to class ethers-buliding-blocks, and the molecular formula is C7H9NO2, Recommanded Product: 2-Amino-3-methoxyphenol.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Comins, Daniel L.; Brown, Jack D. published the artcile< Ortho substitution of m-anisaldehyde via α-amino alkoxide directed lithiation>, Safety of 3-Methoxy-2-methylbenzaldehyde, the main research area is ortho substitution anisaldehyde; amino alkoxide directed lithiation; regioselective lithiation anisaldehyde; methylation anisaldehyde regioselective; methylanisaldehyde.

The directed lithiation of α-amino alkoxides derived from 3-MeOC6H4CHO (I) was studied. The α-amino alkoxides were formed in situ by the addition of I to N-MeLiNCH2CH2NMe2, MeLiNNMe2 or lithium N-methylpiperazide. Several lithiation-methylation reactions of the in situ formed α-amino alkoxides were performed and the products analyzed for 2,3-, 6,3- and 4,3-Me(MeO)C6H3CHO and I. Mixtures of products were obtained in several cases. A highly regioselective directed lithiation occurred at C(2) in C6H6 or PhMe in the presence of MeLiNNMe2 and PhLi. In this manner, 2,3-Me(MeO)C6H3CHO of 96% purity was prepared in 1 step from I in 91% yield.

Journal of Organic Chemistry published new progress about Lithiation, regioselective. 56724-03-9 belongs to class ethers-buliding-blocks, and the molecular formula is C9H10O2, Safety of 3-Methoxy-2-methylbenzaldehyde.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Cho, Hyunkyung; Jeon, Hongjun; Shin, Jae Eui; Lee, Seokwoo; Park, Soojun; Kim, Sanghee published the artcile< Asymmetric synthesis of Cα-substituted prolines through Curtin-Hammett-controlled diastereoselective N-alkylation>, Safety of 3-Methoxy-2-methylbenzaldehyde, the main research area is substituted proline enantioselective diastereoselective synthesis chirality transfer Stevens rearrangement; amino acid proline ester alkylation substituted benzyl; alkylation mechanism Curtin Hammett principle DFT transition state; crystal structure substituted proline quaternization free energy steric effect; Curtin-Hammett principle; chirality transfer; proline derivatives; rearrangement; stereoselectivity.

Asym. synthesis of α-substituted proline derivatives has been accomplished by an efficient chirality-transfer method. High diastereoselectivity of the N-alkylation of the proline ester (C→N chirality transfer) was achieved when a 2,3-disubstituted benzyl group was used as the N-substituent. DFT calculations provided a mechanistic rationale for the high degree of stereoselectivity. The generated N-chirality of the quaternary ammonium salt was transferred back to the α-carbon through a stereoselective [2,3]-Stevens rearrangement (N→C chirality transfer) to give α-substituted proline ester.

Chemistry – A European Journal published new progress about Alkylation, stereoselective. 56724-03-9 belongs to class ethers-buliding-blocks, and the molecular formula is C9H10O2, Safety of 3-Methoxy-2-methylbenzaldehyde.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Kende, Andrew S.; Koch, Kevin published the artcile< Intramolecular radical cyclization of phenolic nitronates. Facile synthesis of annelated tropone and tropolone derivatives>, Electric Literature of 52244-70-9, the main research area is nitrophenolate electron transfer cyclization; spirocyclic nitro dienone preparation rearrangement; bicyclic tropone.

Treating p-HOC6H4(CH2)nNO2 (n = 4, 5) or 4,3-HO(MeO)C6H3(CH2)4NO2 with aqueous KOH followed by K3Fe(CN)6 gives spirocyclic nitrodienones I (X = CH2, CH2CH2; R = H, OMe), which rearrange to bicyclic tropones II (same X, R).

Tetrahedron Letters published new progress about Cycloaddition reaction, intramolecular. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Electric Literature of 52244-70-9.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Noda, Hidetoshi; Asada, Yasuko; Shibasaki, Masakatsu published the artcile< O-Benzoylhydroxylamines as Alkyl Nitrene Precursors: Synthesis of Saturated N-Heterocycles from Primary Amines>, HPLC of Formula: 52244-70-9, the main research area is benzoylhydroxylamine alkyl nitrene precursor primary amine rhodium catalyst; synthesis saturated nitrogen heterocycle.

We introduce O-benzoylhydroxylamines as competent alkyl nitrene precursors. The combination of readily available, stable substrates and a proficient rhodium catalyst provides a straightforward means for the construction of various pyrrolidine rings from the corresponding primary amines. Preliminary mechanistic investigation suggests that the structure of the nitrene precursor plays a role in determining the nature of the resulting reactive intermediate.

Organic Letters published new progress about C-H bond activation. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, HPLC of Formula: 52244-70-9.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem