Month: October 2022

Manohar, Smitha; Sharma, J. N.; Shah, B. V.; Wattal, P. K. published the artcile< Process development for bulk separation of trivalent actinides and lanthanides from radioactive high-level liquid waste>, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide, the main research area is actinide lanthanide solvent extraction radioactive liquid waste.

Inhouse R and D studies resulted in the development of processes for the bulk separation of trivalent actinides and lanthanides from radioactive high-level liquid waste. Synthesis of solvents, namely, n-octyl (phenyl)-N,N-di-iso-Bu carbamoyl Me phosphine oxide and diglycolamide-based tetra (2-ethylhexyl) diglycolamide (TEHDGA), at the required purity was carried out, and a suitable process for their resp. use in actual application was developed. Inactive scale engineering runs comprised of simultaneous extraction and stripping operations were carried out to establish the process on an engineering scale, including reuse of the solvent system. The composition of surrogate high-level waste (HLW) used at engineering-scale studies corresponds to 1st-cycle raffinate from reprocessing of long-cooled pressurized D2O reactor fuel with a burnup of 6500 MWd/ton. Since trivalent lanthanides and actinides exhibits similar extraction behavior at higher acidity, Ce and La were only used in making surrogate HLW to represent all the trivalent lanthanides and actinides. Indigenously developed mixer-settlers using a passive system of mixing were used for these runs. Over a period of ∼10 h, ∼ 300 e of surrogate HLW solutions were contacted with solvent. The results of such repeated trials showed near-total removal of Ce and La (>99.8% and 97%, resp.) at aqueous-to-organic ratio of 2.5:1 for a TEHDGA system. As the distribution coefficient values for trivalent actinide (241Am) are significantly higher than those for trivalent lanthanides for both of the solvent systems under consideration, it can be inferred that separation of trivalent actinides along with lanthanides could be feasible using these solvent systems.

Nuclear Science and Engineering published new progress about Actinides Role: REM (Removal or Disposal), PROC (Process). 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide.

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

Yin, Yaguang; Kong, Xiuqi; Li, Min; Wang, Jingchao; Dai, Xiaoyu; Zhang, Yunyan; Lin, Weiying published the artcile< Development of an esterase fluorescent probe based on naphthalimide-benzothiazole conjugation and its applications for qualitative detection of esterase in orlistat-treated biosamples>, Application of C29H53NO5, the main research area is ESIPT; Esterase fluorescent probe; Fast response; Orlistat-treated cell imaging; Zebrafish imaging.

Esterase is a large hydrolysis family, and widely distributed in many kinds of cells. It is responsible for multiple physiol. and pathol. functions including metabolism, gene expression. While abnormality of esterase is associated with many pathol. activities in obesity, Wolman′s disease, and cancer. Thereby, it is essential to design an effective tool for esterase in situ detection in biol. systems. Herein, a novel fluorescent probe Y-1 for monitoring esterase in living cells was rationally designed. Probe Y-1 was synthesized by the conjugation between an acetylation of 4-hydroxy naphthalimide and benzothiazole group. Benzothiazole moiety is a typical Excited-state intramol. proton transfer (ESIPT) controller. Acetate group was selected as the responsive site and ESIPT initiator. As the acetate group could block the ESIPT effect, the probe emits no fluorescence under the excitation of 455 nm. When binding with esterase, Y-1 shows distinct fluorescence with the peak at 560 nm with short time when ESIPT is on. Y-1 displays high sensitivity (LOD is 0.216 x 10-3 U/mL), fast response (within 5 min), high selectivity and photostability towards esterase. Furthermore, the %RSD (relative standard deviation) of within-day and day-to-day precision was no more than 13.0% and the accuracy ranged from -6.5 to -12.3%. Kinetics performance of Y-1 indicates that esterase has high affinity and hydrolysis to Y-1. For biol. applications, our probe is a time-dependent visualizing esterase in living HepG2 and CoLo205 cells within 15 min. After the treatment of orlistat (1 and 5 μM) for inhibiting the activity of esterase, the bright fluorescence has also been detected using our probe. Furthermore, it has been successful in monitoring the esterase in zebrafish, the data were consistent with cellular phenomena. Therefore, all these findings indicate that the robust probe Y-1 is a useful qual. tool for detecting esterase in biol. systems.

Analytica Chimica Acta published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application of C29H53NO5.

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

Guerra, Walter D.; Lucena-Agell, Daniel; Hortigueela, Rafael; Rossi, Roberto A.; Fernando Diaz, J.; Padron, Jose M.; Barolo, Silvia M. published the artcile< Design, Synthesis, and in vitro Evaluation of Tubulin-Targeting Dibenzothiazines with Antiproliferative Activity as a Novel Heterocycle Building Block>, Application In Synthesis of 6961-82-6, the main research area is dibenzothiazine preparation antiproliferative SAR cell cycle tubulin inhibitor human; Antiproliferation; dibenzothiazines; drug design; sulfonamides; tubulin inhibitors.

A series of free NH and N-substituted dibenzonthiazines I [R1 = H, F, CF3, Ph; R2 = H, 9-F, 7-Ph, etc.; R3 = H, Me, Bn, etc.] with potential anti-tumor activity from N-aryl-benzenesulfonamides was prepared A biol. test of synthesized compounds was performed in vitro measuring their antiproliferative activity against a panel of six human solid tumor cell lines and its tubulin inhibitory activity. Compounds I [R1 = R2 = H; R3 = SO2C6H5, 4-MeC6H4SO2] showed as the best compounds with promising values of activity (overall range of 2-5.4μM).

ChemMedChem published new progress about Antiproliferative agents. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application In Synthesis of 6961-82-6.

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

Vyas, Vijyesh K.; Knighton, Richard C.; Bhanage, Bhalchandra M.; Wills, Martin published the artcile< Combining Electronic and Steric Effects To Generate Hindered Propargylic Alcohols in High Enantiomeric Excess>, Safety of Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium, the main research area is combining electronic steric effect generate hindered propargylic alc high; asym transfer hydrogenation arylacetylenic ketone Tethered ruthenium catalyst; crystallog arylacetylenic ketone asym transfer hydrogenation.

Tethered ruthenium-TsDPEN complexes have been applied to the catalysis of the asym. transfer hydrogenation of a range of aryl/acetylenic ketones. The introduction of an ortho- substituent to the aryl ring of the substrate results in a reversal of the enantioselectivity, while the introduction of two o-fluoro substituents results in an improvement to the reduction enantioselectivity, as does the replacement of a Ph ring on the alkyne with a trimethylsilyl group. These effects are rationalized as resulting from a change in the steric properties of the aryl ring and the electronic properties of the alkyne which, when matched in the reduction transition state, combine within a “”window”” of substrate/catalyst matching to generate products of high ee.

Organic Letters published new progress about Absolute configuration. 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Safety of Chloro[N-[(1R,2R)-1,2-diphenyl-2-[[3-(η6-phenyl)propyl]amino-κN]ethyl]-4-methylbenzenesulfonamidato-κN]ruthenium.

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

Wang, Ying; Sarris, Kathy; Sauer, Daryl R.; Djuric, Stevan W. published the artcile< An expeditious and convenient synthesis of acylsulfonamides utilizing polymer-supported reagents>, Application of C6H6FNO2S, the main research area is acylsulfonamide preparation; acylation sulfonamide carboxylic acid polymer supported reagent.

Acylsulfonamides can be rapidly and conveniently synthesized from a variety of carboxylic acids and sulfonamides utilizing the com. available reagents, PS-DCC and DMAP under mild reaction conditions. DMAP can be efficiently scavenged by utilization of a silica-supported tosic acid cartridge (Si-SCX). In most of the cases studied, products with high purities and yields were obtained without the need for further purification

Tetrahedron Letters published new progress about Acylation. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Application of C6H6FNO2S.

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

Zhang, Cong; Sheng, Lei; Yuan, Ming; Hu, Junjie; Meng, Yan; Wu, Yong; Chen, Liang; Yu, Huifan; Li, Shan; Zheng, Guohua; Qiu, Zhenpeng published the artcile< Orlistat delays hepatocarcinogenesis in mice with hepatic co-activation of AKT and c-Met>, Reference of 96829-58-2, the main research area is orlistat AKT cMet hepatic carcinoma antitumor agent; Fatty acid synthase; Hepatocarcinogenesis; Lipogenesis; Orlistat; Proliferation.

Orlistat (Xenical), a US Food and Drug Administration (FDA)-approved anti-obesity drug, shows efficacy against multiple tumor types, including hepatocellular carcinoma (HCC), due to its ability to inhibit fatty acid synthase (FASN) activity. However, whether orlistat affects hepatocellular malignant transformation during hepatocarcinogenesis in vivo is unknown. This study assessed the antisteatotic and antitumorigenic efficacy of orlistat in a rapid HCC FVB/N mouse model established via hydrodynamic transfection of activated forms of AKT and c-Met proto-oncogenes. Human hepatoma cell lines were used for mech. validation in vitro. Hematoxylin and eosin staining, immunohistochem., and immunoblotting were applied for the mechanistic investigation. The results revealed that when orlistat was administered in the early stage of AKT/c-Met-triggered hepatocarcinogenesis, it resulted in the elimination of hepatic tumor burden. Mechanistically, orlistat efficiently elevated PTEN expression and suppressed AKT/SREBP1/FASN signaling both in vivo and in vitro, impairing AKT/c-Met-driven de novo lipogenesis and aberrant proliferation. Altogether, this study demonstrates the antilipogenic and antiproliferative efficacy of orlistat in hepatocarcinogenesis, suggesting that orlistat may be beneficial for the treatment of HCC, especially in NAFLD-related HCCs featuring activated AKT/mTOR cascade and increased lipogenesis in livers.

Toxicology and Applied Pharmacology published new progress about Antitumor agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Reference of 96829-58-2.

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

Kwon, Yu-Jin; Kwon, Go Eun; Lee, Hye Sun; Choi, Man Ho; Lee, Ji-Won published the artcile< The Effect of Orlistat on Sterol Metabolism in Obese Patients.>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is anti-obesity drug; cardiovascular disease; obesity; orlistat; sterol.

Background: Orlistat, a reversible inhibitor of pancreatic and gastric lipase, is known to have anti-obesity and antioxidant properties. Cholesterol intermediates and metabolites have diverse and important functions in cardiovascular disease. Therefore, we aimed to evaluate the effect of orlistat on sterol metabolism in overweight and obese adults after weight loss during the intervention or weight loss at 12 weeks. Methods: A total of 51 (27 in the control group and 24 in the experimental group), patients with a BMI of 27 or greater were randomly assigned in a 1:1 ratio to receive either orlistat (120 mg) three times a day plus phentermine hydrochloride (37.5 mg) once daily or a placebo three times a day plus phentermine hydrochloride (37.5 mg) once daily. The primary study outcome was sterol metabolism. Results: The experimental group exhibited significantly decreased metabolic signatures of serum sterols, free cholesterol, sitosterol, 7α-hydroxycholesterol (7α-OHC), and 7β-OHC at 12 weeks. The experimental group also exhibited significantly decreased metabolic ratios of sitosterol and 7α-OHC to cholesterol at 12 weeks. Regarding changes in sterol signatures from baseline to 6-month follow-up, free cholesterol, plant sterols, and cholesterol precursors tended to decrease with weight loss during the intervention and increase again as the weight was regained in both groups. Conclusion: Orlistat treatment improves oxysterol metabolism in overweight and obese adults. Our findings support that orlistat plays a crucial role in the process of endothelial dysfunction and atherosclerosis via oxysterol modulation.

Frontiers in endocrinology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Cheng, Dongping; Yan, Xianhang; Pu, Yueqi; Shen, Jing; Xu, Xiaoliang; Yan, Jizhong published the artcile< 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ)-Mediated Tandem Oxidative Annulation for Preparing 2,2-Disubstituted 2,3-Dihydroquinazolin-4(1H)-ones>, Product Details of C7H7BrN2O, the main research area is aminobenzamide diarylpropene DDQ tandem oxidative annulation; dihydroquinazolinone preparation.

An efficient tandem oxidative annulation for the synthesis of 2,2-disubstituted 2,3-dihydroquinazolin-4(1H)-ones via DDQ-mediated dual cross-dehydrogenative-coupling (CDC) reactions is described. This transformation proceeds from easily available o-aminobenzamides and 1,3-diarylpropenes under mild conditions, and the corresponding products are obtained in moderate to excellent yields.

European Journal of Organic Chemistry published new progress about Aryl alkenes Role: RCT (Reactant), RACT (Reactant or Reagent) (1,3-diarylpropenes). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Product Details of C7H7BrN2O.

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

Jia, Yibo; Li, Lin; Duan, Lili; Li, Yue-Ming published the artcile< The aza-Prins Cyclization of Unfunctionalized Olefins Promoted by NHC-Cu Complex and ZrCl4>, Related Products of 6961-82-6, the main research area is piperidine preparation diastereoselective zirconium tetrachloride NHC copper catalyst; homoallylic amine aldehyde aza Prins cyclization.

The aza-Prins cyclization reaction catalyzed by ZrCl4 and NHC (N-heterocyclic carbene) metal complexes is firstly reported. NHC-copper complexes as promoter and ZrCl4 as chloride source are utilized under a mild condition, where homoallylic amines and aldehydes are successfully converted to piperidine derivatives in satisfactory yields and diastereoselectivity.

Applied Organometallic Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Related Products of 6961-82-6.

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

Wu, Kui; Li, Yajun published the artcile< Solid-liquid phase equilibrium and solution thermodynamics of 2-chlorobenzenesulfonamide in 16 mono solvents at temperature ranging from 273.15 K to 324.65 K>, Application In Synthesis of 6961-82-6, the main research area is chlorobenzenesulfonamide solid liquid phase equilibrium solution thermodn.

The synthesis and separation processes of chem. intermediate is based on the knowledge of its solid-liquid phase equilibrium with solvents in industry. In this work, the solubility of 2-chlorobenzenesulfonamide in 16 single pure solvents including methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, acetone, 2-butanone, 2-pentanone, cyclohexanone, cyclopentanone, Et acetate, Me acetate, Et formate, acetonitrile and THF was determined at temperature range from 273.15 to 324.65 K and atm. pressure. The mole fraction solubility of 2-chlorobenzenesulfonamide in all selected mono solvents was enhanced by an increase in temperature In addition, the exptl. data were further correlated by the modified Apelblat equation, λh equation, NRTL model and Wilson model. The values of RAD with NRTL equation were smaller than those with other three models, and thus the NRTL model offered the best fitting performance. The thermodn. functions of dissolution including enthalpy, entropy, and Gibbs energy were derived, and the results expectedly suggested a spontaneous and entropy-driven mixing process. All the crystallog. and thermodn. data reported in this study provides the fundamental data for designing and optimizing of the reaction and crystallization processes of 2-chlorobenzenesulfonamide.

Journal of Molecular Liquids published new progress about Crystallization. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application In Synthesis of 6961-82-6.

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