Month: December 2022

Cai, Yingying published the artcileDouble allylic defluorinative alkylation of 1,1-bisnucleophiles with (trifluoromethyl)alkenes: construction of all-carbon quaternary centers, Application In Synthesis of 864725-22-4, the publication is Organic Chemistry Frontiers (2020), 7(10), 1260-1265, database is CAplus.

A double allylic defluorinative alkylation reaction of 1,1-bisnucleophiles such as C₆H₅CH₂ R (R = H, Ph, C(O) C₆H₅, C(O)OEt, etc.), nitriles R¹CH₂CN (R¹ = Ph, thiophen-2-yl, n-decyl, etc.)and indolin-2-one with (trifluoromethyl)alkenes CH₂=C(R²)CF₃ (R² = Ph, naphthalen-2-yl, pyridin-3-yl, etc.) is reported that occurs via the exclusively regioselective SN2 reaction. Various aliphatic nitriles, esters, and indolin-2-one derivatives could serve as 1,1-bisnucleophiles, delivering diverse attractive sym. gem-difluoroalkene substituted products e.g., I in high yields via the construction of all-carbon quaternary centers. Interestingly, the chemoselective SNV reaction between gem-difluoroalkenes and nucleophiles is completely inhibited. The nitrile group might help to stabilize the α-carbanion intermediates.

Organic Chemistry Frontiers published new progress about 864725-22-4. 864725-22-4 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Alkenyl,Benzene, name is 1,3-Dichloro-5-(3,3,3-trifluoroprop-1-en-2-yl)benzene, and the molecular formula is C9H5Cl2F3, Application In Synthesis of 864725-22-4.

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

Wang, Ming-bo published the artcileSynthesis and structure-activity relationship of novel tetrahydrobenzo[d]thiazole as androgen receptor modulator, Related Products of chlorides-buliding-blocks, the publication is Zhongguo Shengwu Huaxue Yu Fenzi Shengwu Xuebao (2018), 34(9), 962-971, database is CAplus.

Prostate cancer is one of the most commonly diagnosed cancer in men, and androgen receptor (AR) is an important target for the treatment of prostate cancer. For many reasons, existing AR antagonists fail to treat prostate cancer after long-term use. Therefore, the development of novel AR antagonists is still of great significance. A series of tetrahydrobenzo[d]thiazole compounds were synthesized by condensation reaction of α,β-epoxycyclohexanones and appropriate substituted thioureas 8, which were obtained from the corresponding anilines 7. Their antiandrogenic activities were tested using an yeast two-hybrid (Y2H) system, and several compounds exhibited androgen receptor (AR) antagonistic behavior equal or stronger than that of flutamide (IC₅₀ ≤ 2.48 mmol/L). Further cell viability assay demonstrated that some active compounds effectively inhibited the proliferation of androgen-sensitive LNCaP cells values with IC₅₀ values of 17.1-41.4 mmol/L. Mol. docking study provide a possible model of ligand receptor interactions, which was consistent with the initial structure-activity relationship (SAR) studies. Taken together, tetrahydrobenzo[d]thiazoles act as effective AR modulators may represent promising leads for further development of novel and improved AR antagonists.

Zhongguo Shengwu Huaxue Yu Fenzi Shengwu Xuebao published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C10H16Br3N, Related Products of chlorides-buliding-blocks.

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

Galatenko, N. A. published the artcileStudy of the properties of a plastic composition for bone tissue with antiseptic action, Formula: C38H74Cl2N2O4, the publication is Dopovidi Natsional’noi Akademii Nauk Ukraini (2005), 128-133, database is CAplus.

The polymeric composition containing bioactive components and an antiseptic were developed for bone implants. By changing the structure and content of osteoapatite, it was possible to achieve the regulation of the durability of a composite and the output of a medical substance from the polyurethane matrix.

Dopovidi Natsional’noi Akademii Nauk Ukraini published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, Formula: C38H74Cl2N2O4.

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

Galatenko, N. A. published the artcilePolyurethane composition for osteoplasty with antiseptic activity and its properties, Related Products of chlorides-buliding-blocks, the publication is Plasticheskie Massy (2008), 51-54, database is CAplus.

The goal of the present work was to create an osteoplasty composite with prolonged antiseptic action. The composite comprised biocompatible and biodegradable polyurethane, calcium phosphate bioactive filler osteoapatite, antiseptic agent decamethoxine and polymerization catalyst 2,4,6-tris-dimethylaminomethylphenol. The combination of materials used allowed for regulation of the desired properties of the composite.

Plasticheskie Massy published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, Related Products of chlorides-buliding-blocks.

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

Galatenko, N. A. published the artcileStudy of properties of a composition for osteoplasty with decamethoxine, Category: chlorides-buliding-blocks, the publication is Polimernii Zhurnal (2005), 27(3), 202-206, database is CAplus.

A polymeric composite for osteoplasty, characterized by prolonged antibacterial activity was prepared and its properties investigated. The composition comprised a biocompatible, biodegradable base, a calcium phosphate-based ceramic filler, decamethoxine antibacterial agent, and 2,4,6-tris(dimethylaminomethyl)-phenol polymerization accelerator. The base (oligoether urethane diisocyanate) was obtained from 2,4(2,6)-tolylene diisocyanate (T80) and polypropylene glycol. The effects of hydroxyapatite filler and decamethoxine on the structural properties of the composition were studied by IR-spectroscopic and photometric methods and cohesive strength testing. By changing amounts of the components and physicochem. properties of the filler (particle or granule size, percentage of glassy phase, and mass percentage of calcium), it was possible to obtain the material with necessary strength and antibacterial activity required for application in orthopedic surgery.

Polimernii Zhurnal published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, Category: chlorides-buliding-blocks.

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

De Schutter, Joris W. published the artcileNovel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase, Safety of 2-Chloroisonicotinic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(19), 5781-5786, database is CAplus and MEDLINE.

A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhibitors into the isopentenyl pyrophosphate (IPP) and the geranyl pyrophosphate (GPP) substrate sub-pockets of the enzyme are presented.

Bioorganic & Medicinal Chemistry Letters published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Safety of 2-Chloroisonicotinic acid.

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

Bolotov, V. V. published the artcileIonometric identification of methoxine in the medical formulations, HPLC of Formula: 38146-42-8, the publication is Visnik Farmatsii (2003), 30-33, database is CAplus.

We have elaborated the method of express quant. decamethoxine identification in ophthalmic drops, ointments, alc. solution, and tablets by potentiometry methods with the usage of early offered decamethoxine-selective, electrode as indicator. The relative error of identification was 2,0-7,9% in solutions, 4,1-4,2% in ointments, 3,9-4,4% in tablets.

Visnik Farmatsii published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, HPLC of Formula: 38146-42-8.

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

Sbenati, Rawan M. published the artcileDesign, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells, Computed Properties of 32333-53-2, the publication is European Journal of Medicinal Chemistry (2021), 113081, database is CAplus and MEDLINE.

Sorafenib is one of the clin. used anticancer agents that inhibits several kinases. In this study, novel indole-based rigid analogs of sorafenib were designed and synthesized in order to enhance kinase selectivity and hence minimize the side effects associated with its use. The target compounds possess different linkers; urea, amide, sulfonamide, or thiourea, in addition to different terminal aryl moieties attached to the linker in order to investigate their impact on biol. activity. They were tested against Hep3B, Huh7, and Hep-G2 hepatocellular carcinoma (HCC) cell lines to study their potency. Among all the tested target derivatives, arylaminocarbonylaminoindolylpicolinamide I exerted superior antiproliferative potency against all the three tested HCC cell lines compared to sorafenib. Based on these preliminary results, I was selected for further biol. and in silico investigations. Up to 30μM, I did not inhibit 50% of the proliferation of WI-38 normal cells, which indicated promising selectivity against HCC cells than normal cells. In addition, I exerted superior kinase selectivity than sorafenib. It is selective for VEGFR2 and VEGFR3 angiogenesis-related kinases, while sorafenib is a multikinase inhibitor. Superior kinase selectivity of I to sorafenib can be attributed to its conformationally-restricted indole nucleus and the bulky N-methylpiperazinyl moiety. Western blotting was carried out and confirmed the ability of I to inhibit VEGFR2 kinase inside Hep-G2 HCC cells in a dose-dependent pattern. I induces apoptosis and necrosis in Hep-G2 cell line, as shown by caspase-3/7 and lactate dehydrogenase (LDH) release assays, resp. Moreover, I did not inhibit hERG. Thus, we could achieve a more selective kinase inhibitor than sorafenib with retained or even better antiproliferative potency against HCC cell lines. Furthermore, mol. docking and dynamic simulation studies were carried out to investigate its binding mode with VEGFR2 kinase. The mol. has a unique orientation upon binding with the kinase.

European Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Computed Properties of 32333-53-2.

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

Ladelta, Viko published the artcileTetracrystalline Tetrablock Quarterpolymers: Four Different Crystallites under the Same Roof, Synthetic Route of 5034-06-0, the publication is Angewandte Chemie, International Edition (2019), 58(45), 16267-16274, database is CAplus and MEDLINE.

Multicrystalline block polymers having three or more crystalline segments are essential materials for the advancement of physics in the field of crystallinity. The challenging synthesis of multicrystalline polymers has resulted in only a limited number of tricryst. terpolymers having been reported to date. We report, for the first time, the synthesis of polyethylene-b-poly(ethylene oxide)-b-poly(ε-caprolactone)-b-poly(L-lactide) (PE-b-PEO-b-PCL-b-PLLA), a tetracryst. tetrablock quarterpolymer, by combining polyhomologation, ring-opening polymerization, and an organic/metal “catalyst switch” strategy. ¹H NMR spectroscopy and gel-permeation chromatog. confirmed the formation of the tetrablock quarterpolymer, while differential scanning calorimetry, X-ray diffraction, and wide-line separation solid-state NMR spectroscopy revealed the existence of four different crystalline domains.

Angewandte Chemie, International Edition published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Synthetic Route of 5034-06-0.

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

Ladelta, Viko published the artcileA new tricrystalline triblock terpolymer by combining polyhomologation and ring-opening polymerization. synthesis and thermal properties, Application In Synthesis of 5034-06-0, the publication is Journal of Polymer Science, Part A: Polymer Chemistry (2019), 57(24), 2450-2456, database is CAplus.

New tricryst. triblock terpolymers, polyethylene-block-poly(ε-caprolactone)-block-poly(L-lactide) (PE-b-PCL-b-PLLA), were synthesized by ROP of ε-caprolactone (CL) and L-lactide (LLA) from linear ω-hydroxyl polyethylene (PE-OH) macroinitiators. The linear PE-OH macroinitiators were prepared by C1 polymerization of Me sulfoxonium methylide (polyhomologation). Tin(II) 2-ethylhexanoate was used as the catalyst for the sequential ROP of CL and LLA in one-pot polymerization at 85 °C in toluene (PE-OH macroinitiators are soluble in toluene at 80 °C). ¹H NMR spectra confirmed the formation of PE-b-PCL-b-PLLA triblock terpolymers through the appearance of the characteristic proton peaks of each block. GPC traces showed the increase in the number average mol. weight from PE-OH macroinitiator to PE-b-PCL, and PE-b-PCL-b-PLLA corroborating the successful synthesis. The existence of three crystalline blocks was proved by DSC and XRD spectroscopy.

Journal of Polymer Science, Part A: Polymer Chemistry published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C3H9ClOS, Application In Synthesis of 5034-06-0.

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