Month: October 2022

Clive, Derrick L. J.; Peng, Jianbiao; Fletcher, Stephen P.; Ziffle, Vincent E.; Wingert, David published the artcile< Synthesis of Diverse 2,3-Dihydroindoles, 1,2,3,4-Tetrahydroquinolines, and Benzo-Fused Azepines by Formal Radical Cyclization onto Aromatic Rings>, HPLC of Formula: 6850-39-1, the main research area is dihydroindole preparation; quinoline benzotetrahydro stereoselective preparation; tetrahydrobenzoazepine preparation; iodophenol chiral amino alc coupling; aryl amino alc stereoselective preparation N protection; hydroxyalkylhydroxyphenyl carbamate stereoselective preparation iodination; hydroxyphenyliodoalkyl carbamate stereoselective preparation oxidation; iodoalkylcyclohexadienyl carbamate stereoselective preparation radical cyclization; hexahydroindole carbamate preparation rearomatization; hexahydroquinoline carbamate stereoselective preparation rearomatization; carbamate hexahydroindole stereoselective preparation Grignard.

2,3-Dihydroindoles, 1,2,3,4-tetrahydroquinolines, e.g., I, and 2,3,4,5-tetrahydrobenzo[b]azepines are available by a process that represents formal radical cyclization onto aromatic rings. Optically pure benzo-fused heterocycles are also accessible by this method. P-Iodophenols, especially those with the phenolic oxygen protected as a MOM-ether, can be coupled with amino alcs. to produce N-aryl amino alcs., which can be converted into the corresponding alkyl iodides in which the nitrogen is protected as a carbamate. These compounds give cross-conjugated ketones after removal of the phenolic protecting group and oxidation with PhI(OAc)2 in the presence of MeOH. The ketones undergo 5-, 6- or 7-exo-trigonal radical cyclization, and then exposure to acid, or sequential treatment with a Grignard reagent and then acid, effects rearomatization to produce the benzo-fused nitrogen heterocycles.

Journal of Organic Chemistry published new progress about Aromatization. 6850-39-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H13NO, HPLC of Formula: 6850-39-1.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tuckey, Robert C.; Tang, Edith K. Y.; Chen, Yunzhi A.; Slominski, Andrzej T. published the artcile< Selective ability of rat 7-Dehydrocholesterol reductase (DHCR7) to act on some 7-Dehydrocholesterol metabolites but not on lumisterol metabolites>, Related Products of 434-16-2, the main research area is 7-dehydrocholesterol reductase; 7-dehydropregnenolone; DHCR7; Lumisterol; Vitamin D3.

7-Dehydrocholesterol reductase (DHCR7) catalyzes the final step of cholesterol biosynthesis in the Kandutsch-Russel pathway, the reduction of 7-dehydrocholesterol (7DHC) to cholesterol. 7DHC can be acted on by a range of other enzymes including CYP27A1 and CYP11A1, as well as by UVB radiation, producing a number of derivatives including hydroxy-metabolites, some of which retain the C7-C8 double bond and are biol. active. These metabolites include lumisterol (L3) which is a stereoisomer of 7DHC produced in the skin by UVB radiation of 7DHC, as well as vitamin D3. The aim of this study was to test whether these metabolites could act as substrates or inhibitors of DHCR7 in rat liver microsomes. To initially screen the ability of these metabolites to interact with the active site of DHCR7, their ability to inhibit the conversion of ergosterol to brassicasterol was measured. Sterols that significantly inhibited this reaction included 7DHC (as expected), 20S(OH)7DHC, 27(OH)DHC, 8DHC, 20S(OH)L3 and 22(OH)L3 but not 7-dehydropregnenolone (7DHP), 25(OH)7DHC, L3 or vitamin D3 and its hydroxyderivatives. Sterols that inhibited ergosterol reduction were directly tested as substrates for DHCR7. 20S(OH)7DHC, 27(OH)DHC and 7-dehydrodesmosterol were confirmed to be substrates, giving the expected product with the C7-C8 double bond removed. No products were observed from 8DHC or 20S(OH)L3 indicating that these sterols are inhibitors and not substrates of DHCR7. The resistance of lumisterol and 7DHP to reduction by DHCR7 in cells will permit other enzymes to metabolise these sterols to their active forms retaining the C7-C8 double bond, conferring specificity to their biol. actions.

Journal of Steroid Biochemistry and Molecular Biology published new progress about 434-16-2. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Related Products of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bunno, Youka; Tsukimawashi, Yuta; Kojima, Masahiro; Yoshino, Tatsuhiko; Matsunaga, Shigeki published the artcile< Metal-Containing Schiff Base/Sulfoxide Ligands for Pd(II)-Catalyzed Asymmetric Allylic C-H Aminations>, Computed Properties of 627-27-0, the main research area is chiral Schiff base sulfoxide ligand preparation; alkenyl oxazolidinone enantioselective preparation; asym allylic CH amination palladium catalyst Schiff base sulfoxide.

Metal-containing Schiff base/sulfoxides was developed as chiral ligands e.g., I, for Pd(II)-catalyzed asym. intramol. allylic C-H amination reactions. The use of metal-containing Schiff base ligands allowed tuning the selectivity and reactivity of Pd(II)-catalyst, whereby a Schiff base-Cu(II)/sulfoxide ligand in combination with Pd(OAc)2 showed best performance. Both internal and terminal alkenes were applicable and the C-H amination products were obtained in up to 91:9 er.

ACS Catalysis published new progress about Allylic amination. 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, Computed Properties of 627-27-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Maines, Lynn W.; Fitzpatrick, Leo R.; Green, Cecelia L.; Zhuang, Yan; Smith, Charles D. published the artcile< Efficacy of a novel sphingosine kinase inhibitor in experimental Crohn's disease>, COA of Formula: C14H8N2Na2O6, the main research area is sphingosine kinase inhibitor ABC294640 colon edema cytokine Crohns disease.

Aim: Activation of sphingosine kinase (SK) is a key response to many inflammatory processes. The present studies test the hypothesis that an orally available SK inhibitor, ABC294640, would be effective in rodent models of Crohn’s disease. Methods: Trinitrobenzene sulfonic acid (TNBS) was administered rectally to mice and rats. Rats were treated with ABC294640 orally alone or in combination with olsalazine and disease progression was monitored. Results: For both rodent species, treatment with ABC294640 attenuated disease progression. Colon samples from the ABC294640-treated animals had improved histol. and cytokine parameters when compared with vehicle-treated animals. The expression of SK was similarly increased in TNBS-treated animals and in human colon tissue specimens from inflammatory bowel disease patients relative to normal, control patients. Conclusions: Sphingosine kinase may be a critical mediator of colonic damage during intestinal inflammation, and pharmacol. inhibitors of this enzyme may prove useful in the treatment of Crohn’s disease.

Inflammopharmacology published new progress about Body weight. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, COA of Formula: C14H8N2Na2O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Park, Ji Yong; Kim, Young Joo; Lee, Ji Youn; Lee, Yun-Sang; Jeong, Jae Min published the artcile< Imaging of the third gasotransmitter hydrogen sulfide using 99mTc-labeled alpha-hydroxy acids>, SDS of cas: 87-73-0, the main research area is alpha hydroxy acid 99mTc hydrogen sulfide gasotransmitter imaging; Glucoheptonate; Gluconate; H(2)S; Hypoxia; Inflammation; Ischemia; Technetium.

Various α-hydroxy acids such as glycolate, L-lactate, D-lactate, D-gluconate, D-glucoheptonate, D-glucuronate, D-glucarate, and citrate were labeled with 99mTc in the presence of stannous chloride. The labeled compounds were incubated with 0.2 mM of NaHS, and reactive sulfur species and then analyzed by ITLC/normal saline to detect the formation of insoluble complex. Matrigels containing various concentrations of NaHS were xenografted on the shoulder of normal mice, and an imaging study was performed after i.v. injection of [99mTc]Tc-gluconate. We also obtained autoradiog. image of a rat brain with a temporary brain ischemia after i.v. injection of [99mTc]Tc-gluconate.[99mTc]Tc-gluconate showed the highest formation of insoluble complex (87.8 ± 3.6%) after incubation with 0.2 mM NaHS. The Matrigel containing 2μmol NaHS showed uptake of [99mTc]Tc-gluconate, which proved the feasibility as the specific H2S imaging agent in vivo. Temporary ischemic lesion of rat brain showed high radioactivity accumulation representing the feasibility as endogenous H2S imaging agents. We proved that 99mTc-labeled α-hydroxy acid especially [99mTc]Tc-gluconate is a novel endogenous H2S imaging agent, which might contribute to study and diagnosis of various diseases related with inflammation and hypoxia.

Nuclear Medicine and Biology published new progress about Brain. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, SDS of cas: 87-73-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wang, Huamin; Bellotti, Peter; Zhang, Xiaolong; Paulisch, Tiffany O.; Glorius, Frank published the artcile< A base-controlled switch of SO2 reincorporation in photocatalyzed radical difunctionalization of alkenes>, Application of C4H8O, the main research area is trifluoromethylated sulfonyl ketone preparation chemoselective photochem; alkene radical difunctionalization photocatalyst.

Control of selectivity is a pivotal challenge in radical chem. owing to the high reactivity and instability of radical species. Herein, a switchable, base-controlled strategy toward the reincorporation/release of SO2 in photocatalyzed radical difunctionalization of alkenes has been described. By this chemodivergent strategy, a variety of valuable, otherwise difficult-to-access γ-trifluoromethylated ketones and trifluoromethylated sulfonyl ketones can be selectively furnished from the same starting materials. This method features high chemoselectivity, a broad substrate scope, excellent functional group tolerance, and facile scale-up and was applied in a one-pot synthetic procedure. Evaluation of the reaction conditions and mechanistic studies indicate that the choice of base can invert the chemoselectivity of the reaction, demonstrating control over a challenging radical selectivity pattern.

Chem published new progress about Alkenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, Application of C4H8O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bedenko, Stanislav P.; Dement’ev, Konstantin I.; Tret’yakov, Valentin F. published the artcile< Deactivation of Zeolite Catalysts in the Prins Reaction between Propene and Formaldehyde in the Liquid Phase>, SDS of cas: 627-27-0, the main research area is propene formaldehyde zeolite catalyst prins reaction liquid phase.

The Prins reaction between propene and formaldehyde was studied over H-BEA, H-FAU, H-MFI and H-MOR zeolites at 150°C in liquid phase. It was found that the H-BEA sample is the most active and selective toward buta-1,3-diene; the H-MFI is a potential catalyst for 3-buten-1-ol synthesis, while H-FAU can be used for 4-methyl-1,3-dioxane production It had been confirmed that zeolite textural and acidic properties influence catalyst behavior: the acidic properties influence sample activity, while product distribution is controlled by pore volume and effective pore diameter The sample’s deactivation process had been studied and the kinetic model of deactivation was proposed. It was shown that the deactivation rate for the H-MFI catalyst is four times greater than for the H-BEA catalyst, probably because its strong/weak acid sites ratio is much more high than for the H-BEA.

Catalysts published new progress about Catalysts. 627-27-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C4H8O, SDS of cas: 627-27-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Jeong, Eun-mi; Lee, Mi Young; Lee, Jeong Hyun; Lee, Byung Ho; Oh, Kwang-Seok published the artcile< A dual readout assay based on fluorescence polarization and time-resolved fluorescence resonance energy transfer to screen for RSK1 inhibitors>, Computed Properties of 6054-98-4, the main research area is ribosomal S6 kinase 1 inhibitor dual readout assay.

A dual readout assay based on fluorescence polarization (FP) and time-resolved fluorescence resonance energy transfer (TR-FRET) exhibits many advantages over single assay technol. in terms of screening quality and efficiency. In this study, we developed a dual readout assay combining FP and TR-FRET to identify ribosomal S6 kinase 1 (RSK1) inhibitors. This dual readout assay can monitor both FP and TR-FRET signals from a single RSK1 kinase reaction by using the immobilized metal affinity for phosphochem. (IMAP)-based assay. The Z’ value and signal to background (S/B) ratio were 0.85 and 4.0 using FP, and 0.79 and 10.6 using TR-FRET, which led to performance of a pilot library screening against the drug repositioning set consisting of 2320 compounds with a reasonable reproducibility. From this screening, we identified 16 compounds showing greater than 50% inhibition against RSK1 for both FP and TR-FRET; 6 compounds with greater than 50% inhibition only for FP; and 4 compounds with greater than 50% inhibition only for TR-FRET. In a cell-based functional assay to validate the hit compounds, 10 compounds identified only in a single assay had little effect on the RSK-mediated phosphorylation of liver kinase B1, whereas 5 compounds showing greater than 80% inhibition for both FP and TR-FRET reduced the phosphorylation of liver kinase B1. These results demonstrate that the dual readout assay can be used to identify hit compounds by subsequently monitoring both FP and TR-FRET signals from one RSK1 reaction.

Biological & Pharmaceutical Bulletin published new progress about Homo sapiens. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Computed Properties of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Vieira de Castro, Tomas; Yahiaoui, Oussama; Peralta, Ricardo A.; Fallon, Thomas; Lee, Victor; George, Jonathan H. published the artcile< Biomimetic Synthesis Enables the Structure Revision of Littordials E and F and Drychampone B>, Reference of 4396-13-8, the main research area is biomimetic synthesis littordial E F drychampone B; hetero Diels Alder structure revision littordial drychampone.

Structural reassignments for littordial E, littordial F, and drychampone B are proposed on the basis of consideration of their biosynthetic origin. The key step in the proposed biosynthesis of each of these meroterpenoids is an intermol. hetero-Diels-Alder reaction between an o-quinone methide and caryophyllene or humulene. Biomimetic total synthesis of the natural products gave sufficient material to allow their structure revision by NMR studies.

Organic Letters published new progress about Biomimetic synthesis. 4396-13-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H6O5, Reference of 4396-13-8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ji, Peng; Zhang, Yueteng; Wei, Yongyi; Huang, He; Hu, Wenbo; Mariano, Patrick A.; Wang, Wei published the artcile< Visible-Light-Mediated, Chemo- and Stereoselective Radical Process for the Synthesis of C-Glyco-amino Acids>, Reference of 4064-06-6, the main research area is homolytic coupling glycoside glycopeptide preparation; stereoselective C glycosylation photoredox catalyzed imine glycopeptide; imino ester chemoselective addition nucleophilic glycosyl radical amino acid.

An approach for efficient synthesis of C-glycosyl amino acids is described. Different from typical photoredox-catalyzed reactions of imines, the new process follows a pathway in which α-imino esters serve as electrophiles in chemoselective addition reactions with nucleophilic glycosyl radicals. The process is highlighted by the mild nature of the reaction conditions, the highly stereoselectivity attending C-C bond formation, and its applicability to C-glycosylations using both armed and disarmed pentose and hexose derivatives

Organic Letters published new progress about Amino acids Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 4064-06-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H20O6, Reference of 4064-06-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts