Tag: M.W=200-250

Gaile, I. published the artcile2′-Amino-5,5-dimethylcyclohexan-1-one[2,3:4′,5′]thiazole, Category: chlorides-buliding-blocks, the publication is Doklady Akademii Nauk SSSR (1962), 817-19, database is CAplus.

cf. Schulmann, CA 43, 7004i. Refluxing 2-bromodimedon with SC(NH₂)₂ in EtOH 2 hrs., followed by concentration and addition of NH₄OH to pH 8 and addition of H₂O gave 84% 2′-amino-5,5-dimethyl-cyclohexan-1-one[2,3:4,5′]thiazole (I), m. 207°, which also formed similarly from 2-chlorodimedon or from dimedon refluxed with SC(NH₂)₂ and iodine in EtOH 5 hrs. I.HCl decomposed 225°; picrate decomposed 235°. I and Ac₂O gave the N-acetyl derivative of I, m. 219°; similarly was prepared the N-propionyl derivative of I, m. 212°. I and mixed acid gave in 1 hr. at 0° the N-nitro derivative of I, decomposed 201°. I and Br in dioxane gave the N,N-dibromo derivative of I, decomposed 225-6°. Diazotization of I in 85% H₃PO₄ and treatment with MeOH-PhOH gave 80% II, decomposed 245°.

Doklady Akademii Nauk SSSR 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, Category: chlorides-buliding-blocks.

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

Marciniec, B. published the artcileCatalysis of hydrosilylation. Part XVIII. Pt(PPh₃)₂(CH₂:CH₂) – a versatile catalyst for hydrosilylation of olefins, Synthetic Route of 14799-93-0, the publication is Applied Organometallic Chemistry (1990), 4(1), 27-34, database is CAplus.

Pt(PPh₃)₂(CH₂:CH₂) appeared to be a versatile catalyst in hydrosilylation of alkenes (with 5-22 C atoms) as well as of functionalized alkenes such as allyl chloride, allylamine, allyl methacrylate and vinylsilanes. In comparison with a well-known Speier catalyst or with Pt(PPh₃)₄, this complex is characterized by a very high effectiveness (activity and selectivity) and relative resistance to oxygenation and it may be applied in recycling runs with a minor induction period. The catalytic processes examined are of great industrial importance since they lead to a synthesis of alkylsilanes, disilylethanes and silane coupling agents.

Applied Organometallic Chemistry published new progress about 14799-93-0. 14799-93-0 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(methyl)(octyl)silane, and the molecular formula is C9H20Cl2Si, Synthetic Route of 14799-93-0.

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

Xiong, Yusheng published the artcileDiscovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes, COA of Formula: C9H12BClO3, the publication is Journal of Medicinal Chemistry (2012), 55(13), 6137-6148, database is CAplus and MEDLINE.

A potent, selective glucagon receptor antagonist I was discovered by optimization of a previously identified lead. Compound I is a reversible and competitive antagonist with high binding affinity (IC₅₀ of 6.6 nM) and functional cAMP activity (IC₅₀ of 15.7 nM). It is selective for glucagon receptor relative to other family B GPCRs, showing IC₅₀ values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2. Compound I blunted glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowered ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduced glucose (AUC 0-6 h) by 32% and 39% at 3 and 10 mpk single doses, resp. In hGCGR mice on a high fat diet, compound I at 3, and 10 mpk po in feed lowered blood glucose levels by 89% and 94% at day 10, resp., relative to the difference between the vehicle control and lean hGCGR mice. On the basis of its favorable biol. and DMPK properties, compound I (MK-0893) was selected for further preclin. and clin. evaluations.

Journal of Medicinal Chemistry published new progress about 1256345-74-0. 1256345-74-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronic acid and ester, name is (3-Chloro-5-propoxyphenyl)boronic acid, and the molecular formula is C10H15ClO3S, COA of Formula: C9H12BClO3.

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

Ligor, Tomasz published the artcileSorbents for trapping organic pollutants from air, Recommanded Product: Dichloro(methyl)(octyl)silane, the publication is International Journal of Occupational Safety and Ergonomics (1998), 4(2), 153-167, database is CAplus and MEDLINE.

A series of siliceous adsorbents with chem. bonded phases (CBP) of different polarity were tested as sorbents for trapping air pollutants (petroleum ether) using controlled setup. Moreover, special attention was paid to the potential role of metal impurities as strong adsorption sites. Sorbents were characterized by various physico-chem. methods, such as porosimetry, inductively coupled plasma (ICP) anal., elemental anal., derivatog., and gas chromatog. Trapping tubes were utilized for sorption of toxic pollutants from indoor air: VOCs air anal. adsorbents surface characterization gas chromatog.

International Journal of Occupational Safety and Ergonomics published new progress about 14799-93-0. 14799-93-0 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(methyl)(octyl)silane, and the molecular formula is C9H20Cl2Si, Recommanded Product: Dichloro(methyl)(octyl)silane.

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

Garcia-Lopez, Jose-Antonio published the artcileUse of 2-Bromophenylboronic Esters as Benzyne Precursors in the Pd-Catalyzed Synthesis of Triphenylenes, SDS of cas: 1451393-45-5, the publication is Organic Letters (2014), 16(9), 2338-2341, database is CAplus and MEDLINE.

Ortho-Substituted aryl boronates, e.g., I (X= Br, OTf), are introduced as aryne precursors for transition-metal-catalyzed transformations. On treatment with ^tBuOK and Pd(0), metal-bound aryne intermediates are formed that undergo effective trimerization to form useful triphenylene compds, e.g., II. For meta-substituted arynes, the 3:1 product ratio in favor of non-C₃ sym. material is indicative of a benzyne mechanism.

Organic Letters 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, SDS of cas: 1451393-45-5.

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

Giampietro, Letizia published the artcileSynthesis, structure-activity relationships and molecular docking studies of phenyldiazenyl sulfonamides as aromatase inhibitors, Application In Synthesis of 254749-11-6, the publication is European Journal of Medicinal Chemistry (2021), 113737, database is CAplus and MEDLINE.

In this respect, a series of phenyldiazenyl sulfonamides (E)-RS(O)₂NHC₆H₄N=NC₆H₅ (R = Me, Ph, 5-chlorothiophen-2-yl, etc.) and (E)-I was designed, synthesized and tested. Compounds (E)-RS(O)₂NHC₆H₄N=NC₆H₅ (R = 4-cyanophenyl, 2,4-dimethoxyphenyl (II)), and (E)-I (R = 2,4-dimethoxyphenyl) showed an aromatase inhibition in the micromolar range and were evaluated in vitro on the human breast cancer cell line MCF7 by MTT assay, cytotoxicity assay (LDH release), cell cycle anal. and apoptosis, revealing a dose-dependent inhibition profile. In particular, (II) displayed the best reduction in terms of metabolic activity and an anti-proliferative effect on MCF7 cells, being blocked in the G1/S phase checkpoint. Moreover, computational studies were carried out to better understand at a mol. level of detail the rationale behind the effective binding to the active site of aromatase of the more active inhibitor (II). The obtained results allow to consider this compound as an interesting lead for the development of a new class of non-steroidal aromatase inhibitors.

European Journal of Medicinal Chemistry published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C7H3Cl2NO2S, Application In Synthesis of 254749-11-6.

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

Maccallini, Cristina published the artcileNew azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study, Name: 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2021), 36(1), 1631-1644, database is CAplus and MEDLINE.

Nonsteroidal aromatase inhibitors (NSAIs) are well-established drugs for the therapy of breast cancer. However, they display some serious side effects, and their efficacy can be compromised by the development of chemoresistance. Previously, we have reported different indazole-based carbamates and piperidine-sulfonamides as potent aromatase inhibitors. Starting from the most promising compounds, here we have synthesized new indazole and triazole derivatives and evaluated their biol. activity as potential dual agents, targeting both the aromatase and the inducible nitric oxide synthase, being this last dysregulated in breast cancer. Furthermore, selected compounds were evaluated as antiproliferative and cytotoxic agents in the MCF-7 cell line. Moreover, considering the therapeutic diversity of azole-based compounds, all the synthesized compounds were also evaluated as antifungals on different Candida strains. A docking study, as well as mol. dynamics simulation, were carried out to shed light on the binding mode of the most interesting compound into the different target enzymes catalytic sites.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C7H3Cl2NO2S, Name: 2-Chloro-4-cyanobenzene-1-sulfonyl chloride.

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

Wilson, Claire M. published the artcileEnantiospecific sp²-sp³ Coupling of ortho- and para-Phenols with Secondary and Tertiary Boronic Esters, COA of Formula: C6H5BBrClO2, the publication is Angewandte Chemie, International Edition (2017), 56(51), 16318-16322, database is CAplus and MEDLINE.

The coupling of ortho- and para-phenols with secondary and tertiary boronic esters has been explored. In the case of para-substituted phenols, after reaction of a dilithio phenolate species with a boronic ester, treatment with Ph₃BiF₂ or Martin’s sulfurane gave the coupled product with complete enantiospecificity. The methodol. was applied to the synthesis of the broad spectrum antibacterial natural product (-)-4-(1,5-dimethylhex-4-enyl)-2-methylphenol. For ortho-substituted phenols, initial incorporation of a benzotriazole on the phenol oxygen atom was required. Subsequent ortho-lithiation and borylation gave the coupled product, again with complete stereospecificity.

Angewandte Chemie, International Edition 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 C11H8O3, COA of Formula: C6H5BBrClO2.

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

Zhu, Yuting published the artcileAntidiabetic activity and metabolite profiles of ascidian Halocynthia roretzi, Safety of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, the publication is Journal of Functional Foods (2022), 105095, database is CAplus.

Halocynthia roretzi has been cultured and utilized as a nutritious seafood in Southeastern Asia for many years because of its abundance active mols. Here, we reported that feeding of H. roretzi tissues resulted in improving oral glucose tolerance in rats. To screen the active components, we identified 950 chem. compounds from H. roretzi metabolome. Furthermore, 11 mols. with the activity of regulating blood glucose and lipids were selected based on structural identity. Among them, two natural products, hesperetin and astaxanthin were selected for further quant. detection. The results showed that concentrations of hesperetin and astaxanthin in the tissues of H. roretzi were calculated to be 13.7 ± 9.5 and 167.9 ± 48.4μg/100 g, resp. The high content of astaxanthin in H. roretzi indicates its potential roles and functions in anti-diabetes activity. Taken together, our results showed that H. roretzi could be used as a functional food supplement for regulating lipid/glucose metabolism

Journal of Functional Foods 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 C15H23BO2, Safety of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate.

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

Li, Xuefei published the artcileUsing Chlorotrifluoroethane for Trifluoroethylation of (Hetero)aryl Bromides and Chlorides via Nickel Catalysis, Application of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate, the publication is Organic Letters (2021), 23(4), 1400-1405, database is CAplus and MEDLINE.

A nickel-catalyzed reductive cross-coupling between industrial chem. CF₃CH₂Cl and (hetero)aryl bromides and chlorides was reported. The reaction was synthetically simple without the preparation of arylmetals and exhibits high functional group tolerance. The utility of this protocol was demonstrated by the late-stage modification of pharmaceuticals, providing a facile route for medicinal chem.

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, Application of Ethyl 2-(4-chlorophenoxy)-2-methylpropanoate.

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