Tag: M.W=200-250

Yap, Connor published the artcileEnantioselective Nickel-Catalyzed Intramolecular Allylic Alkenylations Enabled by Reversible Alkenylnickel E/Z Isomerization, Quality Control of 480438-56-0, the publication is Angewandte Chemie, International Edition (2017), 56(28), 8216-8220, database is CAplus and MEDLINE.

Enantioselective nickel-catalyzed arylative cyclizations of substrates containing a Z-allylic phosphate tethered to an alkyne are described. These reactions give multisubstituted chiral aza- and carbocycles, and are initiated by the addition of an arylboronic acid to the alkyne, followed by cyclization of the resulting alkenylnickel species onto the allylic phosphate. The reversible E/Z isomerization of the alkenylnickel species is essential for the success of the reactions.

Angewandte Chemie, International Edition published new progress about 480438-56-0. 480438-56-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C7H5ClN2S, Quality Control of 480438-56-0.

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

Ju, Cheng-Wei published the artcileModular Synthesis of Pentagonal and Hexagonal Ring-Fused NBN-Phenalenes Leading to an Excited-State Aromatization-Induced Structural Planarization Molecular Library, Recommanded Product: (2-Bromo-4-chlorophenyl)boronic acid, the publication is Journal of the American Chemical Society (2021), 143(15), 5903-5916, database is CAplus and MEDLINE.

Although polycyclic aromatic hydrocarbons (PAHs) with a nitrogen-boron-nitrogen (NBN) moiety have recently attracted tremendous interest due to their intriguing electronic and optoelectronic properties, all of the NBN-fused π-systems reported to date are called NBN-dibenzophenalenes and were synthesized by electrophilic aromatic substitution. The synthesis of NBN-phenalenes remains challenging, and transition-metal catalysis has never been utilized to construct NBN-embedded π-scaffolds. Herein, a palladium-catalyzed cyclization/bicyclization strategy was developed for the synthesis of diverse pentagonal and hexagonal ring-fused NBN-phenalenes and half-NBN-phenalenes. All of the NBN-embedded π-scaffolds presented in our paper are fluorescent in both solution and the solid state. Further investigations showed that the five-membered NBN rings exhibit the properties of traditional luminogens, while those with a six-membered NBN ring generally undergo photoinduced structural planarization (PISP) and exhibit different colors and quantum yields of fluorescence with different concentrations in solution Time-resolved spectroscopy and TD-DFT calculations revealed that excited-state aromatization is the driving force for PISP in hexagonal ring-fused NBN-π systems, leading to the formation of excimers. Notably, the scope of PISP compounds is still quite limited, and PISP has never been observed in NBN-π systems before. These hexagonal ring-fused NBN-π systems constitute a novel PISP mol. library and appear to be a new class of aggregation-induced excimer emission (AIEE) materials. Finally, the AIEE behavior of these six-membered NBN rings was applied to the detection of nitro explosives, achieving excellent sensitivity. In general, this work provides a new viewpoint for synthesizing NBN-fused π-systems and understanding the excited-state motion of luminogens.

Journal of the American Chemical Society published new progress about 1451393-45-5. 1451393-45-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (2-Bromo-4-chlorophenyl)boronic acid, and the molecular formula is C6H5BBrClO2, Recommanded Product: (2-Bromo-4-chlorophenyl)boronic acid.

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

Liu, Jingbo published the artcileDiscovery of a polysubstituted phenyl containing novel N-phenylpyrazole scaffold as potent ryanodine receptor activator, Recommanded Product: 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, the publication is Bioorganic & Medicinal Chemistry (2020), 28(24), 115829, database is CAplus and MEDLINE.

To develop the novel ryanodine receptors (RyRs) insecticides, encouraged by our previous research work, a series of novel N-phenylpyrazole derivatives containing a polysubstituted Ph ring scaffold were designed and synthesized. The bioassays results indicated that some title compounds exhibited excellent insecticidal activity. For oriental armyworm (Mythimna separata), compounds (I), (II), (III) and (IV) at 0.5 mg L^-1 displayed 100% larvicidal activity, and even at 0.1 mg L^-1, 7o was 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%). Compounds I and IV had the median lethal concentrations (LC₅₀) of 8.83 × 10^-2 and 7.12 × 10^-2 mg L^-1, resp., close to chlorantraniliprole (6.79 × 10^-2 mg L^-1). Addnl., for diamondback moth (Plutella xylostella), the larvicidal activity of compounds I and III were 90% and 70% at 0.01 mg L^-1, resp., better than chlorantraniliprole (50%) and cyantraniliprole (40%). More impressively, the LC₅₀ value of 7f was 4.2 × 10^-3 mg L^-1, slightly lower than that of chlorantraniliprole (5.0 × 10^-3 mg L^-1). The mol. docking between compound I and RyRs of diamondback moth validated our mol. designation. Furthermore, the calcium imaging experiment explored the influence of compound IV on the calcium homeostasis in the central neurons of the third larvae of oriental armyworm. The results of this study indicated that IV is a potent novel lead targeting at RyRs.

Bioorganic & Medicinal Chemistry published new progress about 1869-22-3. 1869-22-3 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Hydrazine,Amine,Benzene, name is 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, and the molecular formula is C7H6ClF3N2, Recommanded Product: 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine.

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

Lin, Chingju published the artcileFenofibrate inhibits hypoxia-inducible factor-1 alpha and carbonic anhydrase expression through activation of AMP-activated protein kinase/ HO -1/Sirt1 pathway in glioblastoma cells, Application of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, the publication is Environmental Toxicology (2021), 36(12), 2551-2561, database is CAplus and MEDLINE.

Cancer and its associated conditions have significant impacts on public health at many levels worldwide, and cancer is the leading cause of death among adults. Peroxisome proliferator-activated receptor α (PPARα)-specific agonists, fibrates, have been approved by the Food and Drug Administration for managing hyperlipidemia. PPARα-specific agonists exert anti-cancer effects in many human cancer types, including glioblastoma (GBM). Recently, we have reported that the hypoxic state in GBM stabilizes hypoxia-inducible factor-1 alpha (HIF-1α), thus contributing to tumor escape from immune surveillance by activating the expression of the pH-regulating protein carbonic anhydrase IX (CA9). In this study, we aimed to study the regulatory effects of the PPARα agonist fibrate on the regulation of HIF-1α expression and its downstream target protein in GBM. Our findings showed that fenofibrate is the high potency compound among the various fibrates that inhibit hypoxia-induced HIF-1α and CA9 expression in GBM. Moreover, fenofibrate-inhibited HIF-1α expression is mediated by HO-1 activation in GBM cells through the AMP-activated protein kinase (AMPK) pathway. In addition, fenofibrate-enhanced HO-1 upregulation activates SIRT1 and leads to subsequent accumulation of SIRT1 in the nucleus, which further promotes HIF-1α deacetylation and inhibits CA9 expression. Using a protein synthesis inhibitor, cycloheximide, we also observed that fenofibrate inhibited HIF-1α protein synthesis. In addition, the administration of the proteasome inhibitor MG132 showed that fenofibrate promoted HIF-1α protein degradation in GBM. Hence, our results indicate that fenofibrate is a useful anti-GBM agent that modulates hypoxia-induced HIF-1α expression through multiple cellular pathways.

Environmental Toxicology published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Application of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate.

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

Thekkeppat, Nipun P. published the artcileCombining Optical Properties with Flexibility in Halogen-Substituted Benzothiazole Crystals, Computed Properties of 19652-33-6, the publication is Crystal Growth & Design (2020), 20(6), 3937-3943, database is CAplus.

Combining optical properties with flexibility in organic crystals may find promising applications in optical waveguides, flexible optoelectronics, etc. We describe a family of halogen-substituted benzothiazole compounds which grow with an acicular needle morphol. based on a slip-stacked supramol. assembly sustained by a series of noncovalent interactions, including halogen bonds etc. Some of them comply with necessary packing features for elasticity; therefore, bending-relaxation cycles can be repeated several times. As these compounds are fluorescent in nature, the optical properties can be gainfully combined with flexibility toward achieving a new class of crystalline materials for optical waveguides and flexible optoelectronics. We describe a family of halogen-substituted benzothiazole compounds which grow with an acicular needle morphol., and some of them are elastically flexible and fluorescent as well. By combining elasticity and optical properties, they will find applications in optical waveguides, flexible optoelectronics, etc.

Crystal Growth & Design published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C9H10O3S, Computed Properties of 19652-33-6.

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

Karimi, Farhad published the artcilePalladium-mediated carboxylation of aryl halides (triflates) or benzyl halides using [¹³C]/[¹¹C]carbon monoxide with tetramethylammonium hydroxide or trimethylphenylammonium hydroxide, Safety of 3-Chloro-2,6-dimethoxybenzoic acid, the publication is Journal of the Chemical Society, Perkin Transactions 1 (2002), 2256-2259, database is CAplus.

[Carbonyl-¹¹C]carboxylic acids were synthesized using palladium-mediated reaction of [¹¹C]carbon monoxide with aryl halides/triflates and benzyl halides in combination with either tetramethylammonium hydroxide or trimethylphenylammonium hydroxide. The radiochem. yields were in the range 20-85%. In a typical experiment starting with 2.1 GBq[¹¹C]carbon monoxide, 0.6 GBq of HPLC-purified 1-[carbonyl-¹¹C]naphthoic acid was obtained within 25 min of the start of the carbonylation reaction (67% decay-corrected radiochem. yield). The specific radioactivity of [carbonyl-¹¹C]nicotinic acid was in the order of 750 GBq μmol^-1 using 10.0 μAh bombardment. [Carbonyl-¹³C]nicotinic acid was synthesized to verify the position of the labeling (δ 166.1) determined by ¹³C NMR.

Journal of the Chemical Society, Perkin Transactions 1 published new progress about 36335-47-4. 36335-47-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Ether, name is 3-Chloro-2,6-dimethoxybenzoic acid, and the molecular formula is C9H9ClO4, Safety of 3-Chloro-2,6-dimethoxybenzoic acid.

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

Delzenne, Gerard A. published the artcilePhotosensitive polymers. I. Synthesis and properties of coumarin-modified polymers, Recommanded Product: Coumarin-6-sulfonyl chloride, the publication is Industrie Chimique Belge (1967), 32(Spec. No.), 373-8, database is CAplus.

Polymers containing intramol. cinnamic esters of the coumarin type were synthesized by treating a poly(hydroxy ether) or partially hydrolyzed poly(vinyl butyral) with 6-coumarincarbonyl chloride, 6-coumarinsulfonyl chloride, or 7-coumarinyl 3-(chlorocarbonyl)-benzenesulfonate. A coumarin-containing copolymer was obtained by copolymerization of Et acrylate and 7-(acryloyloxy)coumarin. The photodimerization of coumarin functions by formation of a cyclobutane structure was useful for imagewise insolubilization of polymers. The photosensitivity of these polymers was compared with the sensitivity of poly(vinyl cinnamate). There was a linear relationship between the light sensitivity of the polymers and the degree of coumarin substitution. The photosensitivity can be enhanced by the addition of sensitizers of the carbonyl type. The more powerful sensitizer seems to be p,p’-bis(dimethylamino)-benzophenone. The sensitization was attributed to a triplet-triplet energy transfer between the light-excited sensitizers and the coumarin units.

Industrie Chimique Belge published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Recommanded Product: Coumarin-6-sulfonyl chloride.

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

Mantell, Mark A. published the artcileS_NAr and C-H Amination of Electron Rich Arenes with Pyridine as a Nucleophile Using Photoredox Catalysis, Synthetic Route of 637-07-0, the publication is Organic Letters (2021), 23(13), 5213-5217, database is CAplus and MEDLINE.

The development of two photocatalytic methods for the pyridination of electron rich arenes was described. First, an SNAr-type reaction between aryl halides and pyridine was developed and optimized. This transformation affords selective substitution of C(sp²)-halogen over C(sp²)-OR bonds to afford arylpyridinium products under anaerobic conditions. Under complementary aerobic conditions, analogous substrates were shown to undergo oxidative C(sp²)-H pyridination.

Organic Letters published new progress about 637-07-0. 637-07-0 belongs to chlorides-buliding-blocks, auxiliary class Inhibitor,Cell Cycle,PPAR, name is Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, and the molecular formula is C12H15ClO3, Synthetic Route of 637-07-0.

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

Prasad, Y. Rajendra published the artcileSynthesis and antimicrobial activity of some novel chalcones of 2-hydroxy-1-acetonaphthone and 3-acetylcoumarin, COA of Formula: C7H4BrClO2, the publication is E-Journal of Chemistry (2006), 3(13), 236-241, database is CAplus.

Five novel chalcones were synthesized by condensing 2-hydroxy-1-acetonaphthone with aldehydes and another five novel chalcones were prepared by refluxing 3-acetylcoumarin with aldehydes in the presence of piperidine in ethanol. All these compounds were characterized by means of their IR, ¹H NMR spectroscopic data and microanalyses. The antimicrobial activity of these compounds was evaluated by the cup plate method.

E-Journal of Chemistry published new progress about 19652-33-6. 19652-33-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Bromide,Benzene,Phenol,Aldehyde, name is 5-Bromo-3-chloro-2-hydroxybenzaldehyde, and the molecular formula is C7H4BrClO2, COA of Formula: C7H4BrClO2.

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

Abdeen, Sanofar published the artcileSulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA), Related Products of chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2018), 61(16), 7345-7357, database is CAplus and MEDLINE.

Extending from a study we recently published examining the anti-trypanosomal effects of a series of GroEL/ES inhibitors based on a pseudo-sym. bis-sulfonamido-2-phenylbenzoxazole scaffold, here, we report the antibiotic effects of asym. analogs of this scaffold against a panel of bacteria known as the ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species). While GroEL/ES inhibitors were largely ineffective against K. pneumoniae, A. baumannii, P. aeruginosa, and E. cloacae (Gram-neg. bacteria), many analogs were potent inhibitors of E. faecium and S. aureus proliferation (Gram-pos. bacteria – EC₅₀ values of the most potent analogs were in the 1-2 μM range). Furthermore, even though some compounds inhibit human HSP60/10 biochem. functions in vitro (IC₅₀ values in the 1-10 μM range), many of these exhibited moderate to low cytotoxicity to human liver and kidney cells (CC₅₀ values >20 μM).

Journal of Medicinal Chemistry published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Related Products of chlorides-buliding-blocks.

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