Tag: M.W=100-150

Hugelshofer, Cedric L. published the artcileCalyciphylline B-Type Alkaloids: Total Syntheses of (-)-Daphlongamine H and (-)-Isodaphlongamine H, Recommanded Product: (S)-2-Methylpropane-2-sulfinamide, the main research area is deoxyisocalyciphylline B structure revision; daphlongamine H total synthesis; isodaphlongamine H total synthesis; Mannich reaction daphlongamine H synthesis; cyclization daphlongamine H synthesis; diastereoselective hydrogenation daphlongamine H synthesis; Pauson Khand reaction daphlongamine H synthesis; calyciphylline B type alkaloid synthesis.

The first total synthesis of the complex hexacyclic Daphniphyllum alkaloid (-)-daphlongamine H (I; 5S,6R) has been accomplished. Key to the success of the strategy are a complexity-building Mannich reaction, efficient cyclizations, and a highly diastereoselective hydrogenation to assemble multigram quantities of the tricyclic core bearing four contiguous stereocenters. Following construction of the hydro-indene substructure by means of a Pauson-Khand reaction, endgame redox manipulations delivered the natural product. Importantly, the synthetic studies have also given access to (-)-isodaphlongamine H (II; 5R,6R) and led to a revision of the reported structure of deoxyisocalyciphylline B as daphlongamine H.

Journal of the American Chemical Society published new progress about Chiral auxiliary (Mannich reaction using sulfinyl imine chiral auxiliary). 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Recommanded Product: (S)-2-Methylpropane-2-sulfinamide.

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

Hamilton, Matthew M. published the artcileDiscovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme, Application In Synthesis of 343338-28-3, the main research area is bicyclohexane preparation indoleamine dioxygenase 1 inhibitor structure activity; structure activity bicyclohexane indoleamine dioxygenase 1 inhibitor.

Indoleamine 2,3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-limiting step in the metabolism of L-tryptophan to kynurenine, has been widely explored as a potential immunotherapeutic target in oncol. The authors have developed a class of inhibitors with a conformationally constrained bicyclo[3.1.0]hexane core. These potently inhibited IDO1 in a cellular context by binding to the apoenzyme, as elucidated by biochem. characterization and X-ray crystallog. A SKOV3 tumor model was instrumental in differentiating compounds, leading to the identification of I (IACS-9779) and II (IACS-70465). IACS-70465 has excellent cellular potency, a robust pharmacodynamic response, and in a human whole blood assay was more potent than linrodostat (BMS-986205). IACS-9779 with a predicted human efficacious once-daily dose below 1 mg/kg to sustain >90% inhibition of IDO1 displayed an acceptable safety margin in rodent toxicol. and dog cardiovascular studies to support advancement into preclin. safety evaluation for human development.

Journal of Medicinal Chemistry published new progress about Crystal structure. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Application In Synthesis of 343338-28-3.

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

Yoshinaga, Yukako published the artcileStereoinvertive C-C Bond Formation at the Boron-Bound Stereogenic Centers through Copper-Bipyridine-Catalyzed Intramolecular Coupling of α-Aminobenzylboronic Esters, Application of (S)-2-Methylpropane-2-sulfinamide, the main research area is bromobenzamidobenzylic boronate nonracemic preparation; isoindolinone nonracemic preparation; copper bipyridine catalyst intramol Suzuki coupling bromobenzamidobenzylic boronate inversion; bipyridine ligand; carbon stereocenters; copper; enantiospecificity; stereospecific reaction.

Nonracemic α-(bromobenzamido)benzylic boronates such as I (R = Me, n-Pr, PhCH2CH2) and ent-I (R = H) underwent stereospecific intramol. Suzuki coupling reactions in the presence of CuCl2 and 2,2′-bipyridine or 6-phenyl-2,2′-bipyridine and mediated by Cs2CO3 and H2O (and in some cases phenol) in toluene/chloroform to yield nonracemic isoindolinones such as II (R = Me, n-Pr, PhCH2CH2) and ent-II (R = H) with inversion of boronate stereochem.

Angewandte Chemie, International Edition published new progress about Cyclization catalysts, stereoselective. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Application of (S)-2-Methylpropane-2-sulfinamide.

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

Das, Pradipta published the artcileDramatic Effect of γ-Heteroatom Dienolate Substituents on Counterion Assisted Asymmetric Anionic Amino-Cope Reaction Cascades, Related Products of amides-buliding-blocks, the main research area is counterion assisted anionic cascade Mannich reaction Cope rearrangement cyclization.

We report a dramatic effect on product outcomes of the lithium ion enabled amino-Cope-like anionic asym. cascade when different γ-dienolate heteroatom substituents are employed. For dienolates with azide, thiomethyl, and trifluoromethylthiol substituents, a Mannich/amino-Cope/cyclization cascade ensues to form chiral cyclohexenone products with two new stereocenters in an anti-relationship. For fluoride-substituted nucleophiles, a Mannich/amino-Cope cascade proceeds to afford chiral acyclic products with two new stereocenters in a syn-relationship. Bromide- and chloride-substituted nucleophiles appear to proceed via the same pathway as the fluoride albeit with the added twist of a 3-exo-trig cyclization to yield chiral cyclopropane products with three stereocenters. When this same class of nucleophiles is substituted with a γ-nitro group, the Mannich-initiated cascade is now diverted to a β-lactam product instead of the amino-Cope pathway. These anionic asym. cascades are solvent- and counterion-dependent, with a lithium counterion being essential in combination with ethereal solvents such as MTBE and CPME. By altering the geometry of the imine double bond from E to Z, the configurations at the R1 and X stereocenters are flipped. Mechanistic, computational, substituent, and counterion studies suggest that these cascades proceed via a common Mannich-product intermediate, which then proceeds via either a chair (X = N3, SMe, or SCF3) or boat-like (X = F, Cl, or Br) transition state to afford amino-Cope-like products or β-lactam in the case of X = NO2.

Journal of the American Chemical Society published new progress about Chiral auxiliary. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Related Products of amides-buliding-blocks.

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

Recommanded Product: 90-16-4. I found the field of Chemistry very interesting. Saw the article Synthesis and Biological Activities of Some New Benzotriazinone Derivatives Based on Molecular Docking; Promising HepG2 Liver Carcinoma Inhibitors published in 2020, Reprint Addresses El Rayes, SM (corresponding author), Suez Canal Univ, Fac Sci, Dept Chem, Ismailia 41529, Egypt.. The CAS is 90-16-4. Through research, I have a further understanding and discovery of Benzo[d][1,2,3]triazin-4(3H)-one.

In one-pot strategy, diazotization of methyl anthranilate 5 followed by addition of amino acid ester hydrochloride, we have prepared methyl-2-(4-oxobenzotriazin-3(4H)-yl)-alkanoates 6a-c. Starting with hydrazides 7a,b, N-alkyl-2-(4-oxobenzotriazin-3(4H)-yl)-alkanamides 9-10(a-h) and methyl-2-(2-(4-oxobenzotriazin-3(4H)-yl)alkanamido)alkanoates 11- 12(a-e) were prepared via azide coupling. Hydrazones 13-15 were prepared via condensation of hydrazides 7a,b with 4-methoxybenzaldehyde, 4-dimethylaminobenzaldehyde, and/or arabinose. Molecular docking was done for synthesized compounds using MOE 2008-10 software. The compounds 9a, 12a, 12c, 13a, 13b, and 14b have the most pronounced strong binding affinities toward the target E. coli Fab-H receptor, whereas compounds 3, 11e, 12e, and 13a have the most pronounced strong binding affinities toward the target vitamin D receptor. The in vitro antibacterial activities of the highest binding affinity docked compounds were tested against E. coli, Staphylococcus aureus, and Salmonella spp. Majority of the tested compounds showed effective positive results against E. coli, while they were almost inactive against Staphylococcus aureus and Salmonella spp. The in vitro cytotoxic activities of the highest binding affinity-docked compounds were tested against the human liver carcinoma cell line (HepG2). Some compounds showed potent cytotoxic activity with low IC50 values, especially for 3 (6.525 mu M) and 13a (10.97 mu M) than that for standard drug doxorubicin (2.06 mu M).

Recommanded Product: 90-16-4. Welcome to talk about 90-16-4, If you have any questions, you can contact El Rayes, SM; Ali, IAI; Fathalla, W; Mahmoud, MAA or send Email.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recently I am researching about AROMATIC POLYAMIDES; MEMBRANES; POLYMERS; CAPTURE, Saw an article supported by the Ministry of Education, Culture, Sports, Science and Technology, JapanMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT) [18K04757]; Japanese Society for the Promotion of ScienceMinistry of Education, Culture, Sports, Science and Technology, Japan (MEXT)Japan Society for the Promotion of Science. Published in ELSEVIER SCI LTD in OXFORD ,Authors: Ito, T; Shiota, R; Taniguchi, N; Spontak, RJ; Nagai, K. The CAS is 104-10-9. Through research, I have a further understanding and discovery of 2-(4-Aminophenyl)ethanol. HPLC of Formula: C8H11NO

In this study, ABA triblock copolymers derived from 4,4′-(hexafluoroisopropylidene)-diphthalic anhydride-2,3,5,6-tetramethyl-1,4-phenylenediamine (6FDA-TeMPD; PI) and 3-hydroxy-1-adamantyl methacrylate (HAdMA) or 3,5-dihydroxy-1-adamantyl methacrylate (DHAdMA) have been synthesized via atom transfer radical polymerization to generate mechanically tough and thermally stable gas-separation membranes with composition-tunable transport properties. Due to the inherent thermodynamic incompatibility between the chemically dissimilar blocks, these two series of triblock copolymers appear microphase-separated. While the gas permeability coefficients of these triblock copolymer membranes are consistently lower than that of PI due to the reduced fractional free volume of HAdMA and DHAdMA, the solubility coefficients of the copolymers are higher than that of PI due presumably to specific interactions between the polar hydroxyl group(s) and penetrant gas molecules. These triblock copolymers synthesized from PI and hydrophilic adamantane derivatives constitute a new class of nanostructured polymeric materials possessing excellent thermomechanical properties in conjunction with designer gas-separation properties.

Welcome to talk about 104-10-9, If you have any questions, you can contact Ito, T; Shiota, R; Taniguchi, N; Spontak, RJ; Nagai, K or send Email.. HPLC of Formula: C8H11NO

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

Salamoun, JM; Garcia, CJ; Hargett, SR; Murray, JH; Chen, SY; Beretta, M; Alexopoulos, SJ; Shah, DP; Olzomer, EM; Tucker, SP; Hoehn, KL; Santos, WL in [Hargett, Stefan R.; Hoehn, Kyle L.] Univ Virginia, Dept Pharmacol, Charlottesville, VA 22908 USA; [Hargett, Stefan R.; Hoehn, Kyle L.] Univ Virginia, Dept Med, Charlottesville, VA 22908 USA; [Chen, Sing-Young; Beretta, Martina; Alexopoulos, Stephanie J.; Shah, Divya P.; Olzomer, Ellen M.; Hoehn, Kyle L.] Univ New South Wales, Sch Biotechnol & Biomol Sci, Kensington, NSW 2033, Australia; [Salamoun, Joseph M.; Garcia, Christopher J.; Murray, Jacob H.; Santos, Webster L.] Virginia Tech, Dept Chem, Blacksburg, VA 24061 USA; [Salamoun, Joseph M.; Garcia, Christopher J.; Murray, Jacob H.; Santos, Webster L.] Virginia Tech, Virginia Tech Ctr Drug Discovery, Blacksburg, VA 24061 USA; [Tucker, Simon P.] Continuum Biosci Pty Ltd, Sydney, NSW 2035, Australia; [Tucker, Simon P.] Continuum Biosci Inc, Boston, MA 02116 USA published 6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Nonalcoholic Steatohepatitis in 2020.0, Cited 93.0. Safety of 2-(4-Aminophenyl)ethanol. The Name is 2-(4-Aminophenyl)ethanol. Through research, I have a further understanding and discovery of 104-10-9.

Small molecule mitochondrial uncouplers have recently garnered great interest for their potential in treating nonalcoholic steatohepatitis (NASH). In this study, we report the structure-activity relationship profiling of a 6-amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol core, which utilizes the hydroxy moiety as the proton transporter across the mitochondrial inner membrane. We demonstrate that a wide array of substituents is tolerated with this novel scaffold that increased cellular metabolic rates in vitro using changes in oxygen consumption rate as a readout. In particular, compound SHS4121705 (12i) displayed an EC50 of 4.3 mu M in L6 myoblast cells and excellent oral bioavailability and liver exposure in mice. In the STAM mouse model of NASH, administration of 12i at 25 mg kg(-1) day(-1) lowered liver triglyceride levels and improved liver markers such as alanine aminotransferase, NAFLD activity score, and fibrosis. Importantly, no changes in body temperature or food intake were observed. As potential treatment of NASH, mitochondrial uncouplers show promise for future development.

Safety of 2-(4-Aminophenyl)ethanol. Welcome to talk about 104-10-9, If you have any questions, you can contact Salamoun, JM; Garcia, CJ; Hargett, SR; Murray, JH; Chen, SY; Beretta, M; Alexopoulos, SJ; Shah, DP; Olzomer, EM; Tucker, SP; Hoehn, KL; Santos, WL or send Email.

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

Authors Chen, FS; Hu, SS; Li, SP; Tang, G; Zhao, YF in ROYAL SOC CHEMISTRY published article about ALKYNE INSERTION; LIGANDS; ACIDS; ANNULATION; 1,2,3-BENZOTRIAZIN-4(3H)-ONES in [Tang, Guo] Xiamen Univ, Dept Chem, Coll Chem & Chem Engn, Xiamen 361005, Fujian, Peoples R China; Xiamen Univ, Key Lab Chem Biol Fujian Prov, Xiamen 361005, Fujian, Peoples R China in 2021, Cited 54. Recommanded Product: 90-16-4. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4

Metal-free, visible-light-induced denitrogenative phosphorylation of 1,2,3-benzotriazinones was achieved. With the use of eosin Y as a photoredox catalyst, N,N-diisopropylethylamine as a base, CH3CN-H2O as a solvent and sunlight or a blue LED as a light source, a variety of aryl-phosphonates, aryl-phosphinates, and aryl-phosphine oxides were efficiently prepared. In addition, B(2)pin(2) instead of P-nucleophiles as a radical acceptor was also demonstrated. The key advantages of this newly developed method are the clean reaction profile, use of a low-cost organic-dye catalyst, energy efficiency, broad substrate scope, good to excellent yields and large-scale synthetic applicability. The gram-scale synthesised compounds could be isolated in pure form just upon extraction, followed by re-crystallisation; no tedious chromatographic purification was required.

Welcome to talk about 90-16-4, If you have any questions, you can contact Chen, FS; Hu, SS; Li, SP; Tang, G; Zhao, YF or send Email.. Recommanded Product: 90-16-4

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Formula: C7H5N3O. Reddy, GS; Snehalatha, AV; Edwin, RK; Hossain, KA; Giliyaru, VB; Hariharapura, RC; Shenoy, GG; Misra, P; Pal, M in [Reddy, Gangireddy Sujeevan; Snehalatha, Ampalam Venkata; Edwin, Rebecca Kristina; Hossain, Kazi Amirul; Misra, Parimal; Pal, Manojit] Dr Reddys Inst Life Sci, Univ Hyderabad Campus, Hyderabad 500046, India; [Reddy, Gangireddy Sujeevan; Giliyaru, Varadaraj Bhat; Hariharapura, Raghu Chandrashekhar; Shenoy, G. Gautham] Manipal Acad Higher Educ, Manipal Coll Pharmaceut Sci, Manipal 576104, Karnataka, India published Synthesis of 3-indolylmethyl substituted (pyrazolo/benzo)triazinone derivatives under Pd/Cu-catalysis: Identification of potent inhibitors of chorismate mutase (CM) in 2019, Cited 38. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4.

The chorismate mutase (CM) is considered as an attractive target for the identification of potential antitubercular agents due to its absence in animals but not in bacteria. A series of 3-indolylmethyl substituted pyrazolo-triazinone derivatives were designed and docked into CM in silico as potential inhibitors. These compounds were efficiently synthesized using the Pd/Cu-catalyzed coupling-cyclization in a single pot involving the construction of indole ring. The methodology was later extended to the preparation of corresponding benzo analogs of pyrazolotriazinones i.e. 3-indolylmethyl substituted benzotriazinone derivatives. Several of these novel compounds showed significant inhibition of CM when tested in vitro at 30 mu M. The SAR (Structure-Activity-Relationship) studies suggested that benzotriazinone moiety was more favorable over the pyrazolotriazinone ring. The two best active compounds showed IC50 similar to 0.4-0.9 mu M (better than the reference/known compounds used) and no toxicity till 30 mu M in vitro.

Formula: C7H5N3O. Bye, fridends, I hope you can learn more about C7H5N3O, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one. Barak, DS; Mukhopadhyay, S; Dahatonde, DJ; Batra, S in [Barak, Dinesh S.; Mukhopadhyay, Sushobhan; Dahatonde, Dipak J.; Batra, Sanjay] CSIR Cent Drug Res Inst, Med & Proc Chem Div, Sect 10,Jankipuram Extens,Sitapur Rd, Lucknow 226031, Uttar Pradesh, India; [Batra, Sanjay] CSIR HRDC, Postal Staff Coll Area, Sect 19, Ghaziabad 201002, India published NaNO2/I-2 as an alternative reagent for the synthesis of 1,2,3-benzotriazin-4(3H)-ones from 2-aminobenzamides in 2019, Cited 39. The Name is Benzo[d][1,2,3]triazin-4(3H)-one. Through research, I have a further understanding and discovery of 90-16-4.

An efficient transformation of 2-aminobenzamides to 1,2,3-benzotriazin-4(3H)-ones in the presence of sodium nitrite (NaNO2) and Iodine (I-2) is described. The reaction is proposed to proceed via formation of nitrosyl halide that induces nitrosylation of the amino group of 2-aminobenzamide leading to diazotization followed by intramolecular cyclization. (C) 2018 Elsevier Ltd. All rights reserved.

Quality Control of Benzo[d][1,2,3]triazin-4(3H)-one. Welcome to talk about 90-16-4, If you have any questions, you can contact Barak, DS; Mukhopadhyay, S; Dahatonde, DJ; Batra, S or send Email.

Reference:
Patent; Guizhou University; Xue Wei; Zhang Juping; Zhang Cheng; Chen Lijuan; Wang Yihui; Li Pu; Li Qin; Ruan Xianghui; Wang Xiaobin; Wu Xiaoqiong; Wang Jun; (24 pag.)CN107602493; (2019); B;,
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics