Tag: M.W=250-300

Korrapati, Vinodh K. published the artcileBilayer coatings for temporary and long-term corrosion protection of magnesium-AZ31 alloy, Formula: C15H20O6, the publication is Progress in Organic Coatings (2022), 106608, database is CAplus.

Phosphate and silane containing organic self-assembled (SA) layers serve as pre-treatments on magnesium alloy sheet materials. A reliable protection was achieved in this work via application of alkyd-based coatings on the pretreated surface. The idea of adopting SA pre-treatments as functional layers at metal-polymer interface is to influence the adhesive properties between solid metal substrate and alkyd-based coating. Hexadecyltrimethoxysilane (HDTMS) deposited metal surfaces exhibit stronger adhesive strength, while a near homogeneous distribution of the octadecylphosphonic acid (ODPA) and perfluorodecylphosphonic acid (PFDPA) exhibit low adhesive phenomenon, when placed as pre-layers in bilayer coatings. Electrochem. impedance results after 168 h of immersion reveal that the organophosphate and organosilane deposited bilayer films demonstrate protective properties with almost no interface defects. Moreover, organophosphate treated bilayer coatings enhance easy peeling of alkyd coat after protecting the surface from corrosive electrolytes. Bilayer coatings developed on AZ31 sheets can confer temporary or long-term corrosion protection depending on further processing strategy and offer efficient alloy protection for both purposes.

Progress in Organic Coatings published new progress about 15625-89-5. 15625-89-5 belongs to esters-buliding-blocks, auxiliary class Polymerization Reagents,Crosslinkers, name is Trimethylolpropane triacrylate, and the molecular formula is C15H20O6, Formula: C15H20O6.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Krushinski, Joseph H. published the artcileIndoloxypropanolamine analogues as 5-HT_1A receptor antagonists, Application In Synthesis of 115314-17-5, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(20), 5600-5604, database is CAplus and MEDLINE.

Analogs of pindolol, 1-(1H-indol-4-yloxy)-3-(isopropylamino)propan-2-ol, were synthesized and evaluated as 5-HT_1A receptor antagonists. The structural features required for optimal binding to the 5-HT1A receptor are as follows: S-2-propanol linker, 4-indoloxy substituent, and a large lipophilic cyclic amine substituent. Compound I is a potent antagonist at the 5-HT₁A receptor. This compoundis not a candidate for further development because of its affinity for the β₁ and β₂ receptors.

Bioorganic & Medicinal Chemistry Letters published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Application In Synthesis of 115314-17-5.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Abdul-Hay, Samer published the artcileNO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor, Safety of (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, the publication is ACS Medicinal Chemistry Letters (2011), 2(9), 656-661, database is CAplus and MEDLINE.

Hybrid nitrate drugs have been reported to provide NO bioactivity to ameliorate side effects or to provide ancillary therapeutic activity. Hybrid nitrate selective serotonin reuptake inhibitors (NO-SSRIs) were prepared to improve the therapeutic profile of this drug class. A synthetic strategy for use of a thiocarbamate linker was developed, which in the case of NO-fluoxetine facilitated hydrolysis to fluoxetine at pH 7.4 within 7 h. In cell culture, NO-SSRIs were weak inhibitors of the serotonin transporter; however, in the forced swimming task (FST) in rats, NO-fluoxetine demonstrated classical antidepressant activity. Comparison of NO-fluoxetine, with fluoxetine, and an NO-chimera nitrate developed for Alzheimer’s disease (GT-1061) were made in the step through passive avoidance (STPA) test of learning and memory in rats treated with scopolamine as an amnesic agent. Fluoxetine was inactive, whereas NO-fluoxetine and GT-1061 both restored long-term memory. GT-1061 also produced antidepressant behavior in FST. These data support the potential for NO-SSRIs to overcome the lag in onset of therapeutic action and provide co-therapy of neuropathologies concomitant with depression.

ACS Medicinal Chemistry Letters published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Safety of (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Adejare, Adeboye published the artcileSynthesis and β-adrenergic activities of R-fluoronaphthyloxypropanolamine, Recommanded Product: (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, the publication is Pharmaceutical Research (1997), 14(4), 533-536, database is CAplus.

Many biogenic amines where an aromatic proton is substituted with fluorine have exhibited pharmacol. properties that are dependent on the position of fluorine on the aromatic ring. For example, 6-fluoroepinephrine is selective for α-adrenergic receptors whereas the 2-fluoroisomer is selective for β-receptors. Aryloxypropanolamines are β-receptor agonists or antagonists, depending on the aryl group and its substituents. The authors therefore hypothesized that fluorine substitution on the aromatic ring could lead to significant biol. effects in this class. A target with fluorine on naphthyl group of a known β-antagonist was chosen for investigation. Synthesis of the target compound began with fluoronaphthalene and involved introduction of 4-hydroxy group by Friedel-Crafts acylation followed by Baeyer Villiger oxidation The side chain was introduced stereoselectively using the chiral synthon (2R)-glycidyl 3-nitrobenzenesulfonate, a Sharpless epoxidation technique. The epoxide was opened with t-Bu amine. HPLC methods were used to characterize %ee of the enantiomer. The target compound was synthesized in several hundred milligram quantity, and in good yield and high enantiomeric excess, showing practicality of the synthetic scheme. It exhibited potent binding activities on β-adrenergic receptors, and was two times selective for β₂-receptors over β₁. The current report demonstrates that aromatic fluorine substitution on β-adrenergic ligands can be achieved, and that such can be used to obtain binding selectivity between β receptors.

Pharmaceutical Research published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Recommanded Product: (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Kunitake, Toyoki published the artcileCatalytic hydrolysis of dinitrophenyl sulfate by polyethylenimine derivatives, Category: esters-buliding-blocks, the publication is Bulletin of the Chemical Society of Japan (1979), 52(8), 2402-8, database is CAplus.

The catalytic hydrolysis of nitrophenyl sulfates by poly(ethylenimine) (PEI) derivatives was investigated at 30° in aqueous buffers. The catalytic hydrolysis of 2-hydroxy-5-nitrophenyl sulfate by an PEI with imidazolylmethyl and dodecyl substituents failed to proceed in spite of the contrary report by Kiefer et al. 2,4-Dinitrophenyl sulfate was cleaved fairly readily by PEI derivatives Simple sulfate transfer was observed in the case of alkylated PEI, but the catalytic hydrolysis proceeded according to the Michaelis-Menten kinetics in the case of quaternized PEI. Partly quaternized PEI’s showed highest catalytic efficiencies reported to date for the hydrolysis of dinitrophenyl sulfate. Nitrophenyl sulfates were not cleaved by these polymers.

Bulletin of the Chemical Society of Japan published new progress about 6217-68-1. 6217-68-1 belongs to esters-buliding-blocks, auxiliary class Salt,Nitro Compound,Sulfonate,Benzene, name is Potassium 4-nitrophenyl sulfate, and the molecular formula is C6H4KNO6S, Category: esters-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Lawer, Aggie published the artcileInternal Nucleophilic Catalyst Mediated Cyclisation/Ring Expansion Cascades for the Synthesis of Medium-Sized Lactones and Lactams, COA of Formula: C15H21BO4, the publication is Angewandte Chemie, International Edition (2019), 58(39), 13942-13947, database is CAplus and MEDLINE.

A strategy for the synthesis of medium-sized lactones and lactams from linear precursors is described in which an amine acts as an internal nucleophilic catalyst to facilitate a novel cyclisation/ring expansion cascade sequence. This method obviates the need for the high-dilution conditions usually associated with medium-ring cyclisation protocols, as the reactions operate exclusively via kinetically favorable “normal”-sized cyclic transition states. This same feature also enables biaryl-containing medium-sized rings to be prepared with complete atroposelectivity by point-to-axial chirality transfer.

Angewandte Chemie, International Edition published new progress about 956229-86-0. 956229-86-0 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Benzene,Ester,Boronate Esters,Boronic acid and ester, name is Methyl 2-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetate, and the molecular formula is C15H21BO4, COA of Formula: C15H21BO4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Karmel, Caleb published the artcileIridium-Catalyzed Silylation of Five-Membered Heteroarenes: High Sterically Derived Selectivity from a Pyridyl-Imidazoline Ligand, Formula: C13H19BO4S, the publication is Angewandte Chemie, International Edition (2020), 59(15), 6074-6081, database is CAplus and MEDLINE.

The steric effects of substituents on five-membered rings are less pronounced than those on six-membered rings because of the difference in bond angles. Thus, the regioselectivities of reactions of five-membered heteroarenes that occur with selectivities dictated by steric effects, such as the borylation of C-H bonds, were poor in many cases. The authors report that the silylation of five-membered-ring heteroarenes occurs with high sterically derived regioselectivity when catalyzed by the combination of [Ir(cod)(OMe)]₂ (cod = 1,5-cyclooctadiene) and a phenanthroline ligand or a new pyridyl-imidazoline ligand that further increases the regioselectivity. The silylation reactions with these catalysts produce high yields of heteroarylsilanes from functionalization at the most sterically accessible C-H bonds of these rings under conditions that the borylation of C-H bonds with previously reported catalysts formed mixtures of products or products that are unstable. The heteroarylsilane products undergo cross-coupling reactions and substitution reactions with ipso selectivity to generate heteroarenes that bear halogen, aryl, and perfluoroalkyl substituents.

Angewandte Chemie, International Edition published new progress about 960116-27-2. 960116-27-2 belongs to esters-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Ester,Thiophene,Boronate Esters,Boronic Acids,Boronic acid and ester,, name is Ethyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)thiophene-3-carboxylate, and the molecular formula is C13H19BO4S, Formula: C13H19BO4S.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Baker, Jennifer R. published the artcileAmino Alcohol Acrylonitriles as Activators of the Aryl Hydrocarbon Receptor Pathway: An Unexpected MTT Phenotypic Screening Outcome, Quality Control of 115314-17-5, the publication is ChemMedChem (2020), 15(6), 490-505, database is CAplus and MEDLINE.

Lead (Z)-N-(4-(2-cyano-2-(3,4-dichlorophenyl)vinyl)phenyl)acetamide, 1 showed MCF-7 GI₅₀=30 nM and 400-fold selective c.f. MCF10A (normal breast tissue). Acetamide moiety modification (13 a-g) to introduce addnl. hydrophobicity was favored with MCF-7 breast cancer cell activity enhanced at 1.3 nM. Other analogs were potent against the HT29 colon cancer cell line at 23 nM. Textbook SAR data was observed in the MCF-7 cell line, in an MTT assay, via the ortho (17 a), meta (17 b) and para (13 f). The amino alc. -OH moiety was pivotal, but no stereochem. preference noted. But, these data did not fit our homol. modeling expectations. Aberrant MTT ((3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) screening results and metabolic interference confirmed by sulforhodamine B (SRB) screening. Interfering analogs resulted in 120 and 80-fold CYP1A1 and CYP1A2 amplification, with no upregulation of SULT1A1. This is consistent with activation of the AhR pathway. Piperidine per-deuteration reduced metabolic inactivation. 3-OH / 4-OH piperidine analogs showed differential MTT and SRB activity supporting MTT assay metabolic inactivation. Data supports piperidine 3-OH, but not the 4-OH, as a CYP substrate. This family of β-amino alc. substituted 3,4-dichlorophenylacetonitriles show broad activity modulated via the AhR pathway. By SRB anal. the most potent analog was 23 b, (Z)-3-(4-(3-(4-phenylpiperidin-1-yl)-2-hydroxypropoxy)phenyl)-2-(3,4-dichlorophenyl)-acrylonitrile.

ChemMedChem published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Quality Control of 115314-17-5.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Duncan, Kenneth W. published the artcileStructure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666, Computed Properties of 115314-17-5, the publication is ACS Medicinal Chemistry Letters (2016), 7(2), 162-166, database is CAplus and MEDLINE.

The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound I (EPZ015666, GSK3235025) to probe the underlying pharmacol. of this key enzyme. Herein, the authors report the design and optimization strategies employed on an initial hit compound with poor in vitro clearance to yield in vivo tool compound I and an addnl. potent in vitro tool mol. II (GSK3203591).

ACS Medicinal Chemistry Letters published new progress about 115314-17-5. 115314-17-5 belongs to esters-buliding-blocks, auxiliary class Epoxides,Chiral,Nitro Compound,Sulfonate,Benzene, name is (R)-Oxiran-2-ylmethyl 3-nitrobenzenesulfonate, and the molecular formula is C9H9NO6S, Computed Properties of 115314-17-5.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics

Yougnia, Rodrigue published the artcileOne-pot synthesis of novel poly-substituted phenanthrenes, Product Details of C15H21BO4, the publication is Tetrahedron (2010), 66(15), 2803-2808, database is CAplus.

A one-pot synthesis of novel poly-substituted phenanthrenes is described in this article through a Suzuki-Miyaura cross-coupling followed by a Dieckmann-Thorpe ring closure under microwave irradiation The selection of the appropriate starting materials allowed us to introduce diversity on various positions of the phenanthrene ring system.

Tetrahedron published new progress about 956229-86-0. 956229-86-0 belongs to esters-buliding-blocks, auxiliary class Boronic acid and ester,Benzene,Ester,Boronate Esters,Boronic acid and ester, name is Methyl 2-(2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)acetate, and the molecular formula is C13H19BO3, Product Details of C15H21BO4.

Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics