Month: October 2022

Bubel, O. N.; Bezborodov, V. S.; Ptashnikov, Yu. L. published the artcile< Synthesis of mesomorphic derivatives of p-aminobenzoic acid>, Synthetic Route of 16426-64-5, the main research area is Schiff base aminobenzoate mesomorphic; liquid crystal aminobenzoate Schiff base.

4-HOC6H4CHO was etherified with RX (R = Me, EtCHMeCH2, m-C5H11, n-C10H21; X = Br, iodo) to give 85-90% 4-ROC6H4CHO, which condensed with 2,4-R1(H2N)C6H3CO2R2 (R1 = H, Cl, Br; R2 = H, EtCHMeCH2, n-C5H11) to give 11 mesomorphic 4-ROC6H4CH:NC6H3(CO2R2)R1-4,3 (I). I (R = R2 = EtCHMeCH2, R1 = H) exists as a mixture of the crystalline and isotropic phases; the other I also exists as smectic liquid-crystalline A or C phases or as nematic liquid crystals.

Zhurnal Organicheskoi Khimii published new progress about Liquid crystals. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Synthetic Route of 16426-64-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Abram, Michal; Rapacz, Anna; Mogilski, Szczepan; Latacz, Gniewomir; Lubelska, Annamaria; Kaminski, Rafal M.; Kaminski, Krzysztof published the artcile< Multitargeted Compounds Derived from (2,5-Dioxopyrrolidin-1-yl)(phenyl)-Acetamides as Candidates for Effective Anticonvulsant and Antinociceptive Agents>, Recommanded Product: (3-Bromophenyl)(trifluoromethyl)sulfane, the main research area is epilepsy neuropathic pain anticonvulsant antinociceptive multitargeted drugs hybrid compound; Hybrid compounds; anticonvulsant activity; antinociceptive activity; epilepsy; multitargeted drugs; neuropathic pain.

We developed a focused set of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant and antinociceptive properties. These hybrid compounds demonstrated broad-spectrum protective activity in a range of mouse models, such as the maximal electroshock (MES) test, the pentylenetetrazole-induced seizures (scPTZ), and the 6 Hz (32 mA) seizures. Compound 22(I) showed the most potent anticonvulsant activity (ED50 MES = 23.7 mg/kg, ED50 6 Hz (32 mA) = 22.4 mg/kg, ED50scPTZ = 59.4 mg/kg). In addition, 22 revealed potent efficacy in the formalin-induced tonic pain. These in vivo activities of 22 are likely mediated by several targets and may result from the inhibition of central sodium/calcium currents and transient receptor potential vanilloid 1 (TRPV1) receptor antagonism. Finally, the lead compound 22 revealed drug-like absorption, distribution, metabolism, excretion, toxicity (ADME-Tox) properties in the in vitro assays, making it a potential candidate for further development in epilepsy and neuropathic pain indications.

ACS Chemical Neuroscience published new progress about Analgesics. 2252-45-1 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3S, Recommanded Product: (3-Bromophenyl)(trifluoromethyl)sulfane.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Sharma, Mukesh; Das, Biraj; Baruah, Manash J.; Biswas, Subir; Roy, Subhasish; Hazarika, Anil; Bhargava, Suresh K.; Bania, Kusum K. published the artcile< Pd-Au-Y as Efficient Catalyst for C-C Coupling Reactions, Benzylic C-H Bond Activation, and Oxidation of Ethanol for Synthesis of Cinnamaldehydes>, Name: 3-(4-Bromophenyl)acrylaldehyde, the main research area is phenylboronic acid aryl chloride palladium gold nanocatalyst Suzuki Miyaura; biaryl one pot preparation; benzylic alc chloride palladium gold nanocatalyst oxidation; benzaldehyde preparation; acetaldehyde benzaldehyde chloride palladium gold nanocatalyst aldol condensation; cinnamaldehyde preparation.

Pd-Au nanoalloy supported on zeolite-Y (Pd-Au-Y) matrix was found to be an effective catalyst for C-Cl bond activation and oxidative coupling of 2-naphthol, leading to the formation of various biaryl products and 1,1′-bi-2-naphthol, BINOL. The same catalyst was also highly efficient for selective oxidation of benzylic alcs. to benzaldehydes. Cinnamaldehydes were obtained directly from benzaldehydes by aldol condensation with acetaldehyde generated in situ by partial oxidation of ethanol in the presence of Pd-Au-Y catalyst at 120 °C under basic condition. The biaryl products were also obtained directly from benzylic alcs. in a one-pot system by reacting with phenylboronic acid. The formation of biaryls from benzylic alcs. was believed to occur via one-pot benzylic C-H and C-Cl bond activation. A high % yield of biaryls, BINOL, aldehydes, and cinnamaldehydes was obtained by performing different reactions using the single Pd-Au-Y catalyst. The strong interaction of chloro-benzylic alc. was predominantly located at active gold species. X-ray photoelectron and diffuse reflectance spectroscopic studies revealed the strong interaction between Pd and Au particles. Electrochem. studies provided proper evidence for the individual role of the nanoparticles (NPs) in one-pot synthesis of biaryls from benzylic alcs.

ACS Catalysis published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Name: 3-(4-Bromophenyl)acrylaldehyde.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Das, Anupam; Thomas, K. R. Justin published the artcile< Light Promoted Synthesis of Quinoxalines and Imidazo[1,2-a]pyridines via Oxybromination from Alkynes and Alkenes>, Synthetic Route of 20099-90-5, the main research area is quinoxaline preparation green chem; alkyne phenylenediamine photochem heterocyclization; imidazopyridine preparation green chem; alkene aminopyridine photochem heterocyclization.

Light promoted two-step one-pot syntheses of quinoxalines I (R1 = H, Ph; R2 = Me, Cl, CN, etc.) and imidazo[1,2-a]pyridines II (R3 = 4-Me, 2-Br, 4-NO2, etc.) from alkynes 4-R2C6H4CCR1 and alkenes R3C6H4CH=CH2, resp. under mild conditions are described. The conversions occur via the formation of α,α’-dibromo ketones 4-R2C6H4C(O)C(Br)2R1 or α-bromo ketones R3C6H4C(O)CH2Br on irradiation with UV LED fluorescent black light (380-390 nm) in acetonitrile/water mixture This protocol does not require sensitizer or catalyst or additives. This two-step protocol is a new entry of synthetic methods available for quinoxaline derivatives I and imidazopyridine derivatives II and offers wide functional group tolerance.

Asian Journal of Organic Chemistry published new progress about Alkynes, aryl Role: RCT (Reactant), RACT (Reactant or Reagent). 20099-90-5 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO3, Synthetic Route of 20099-90-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Li, Yaxuan; Fu, Yajie; Ren, Chaojie; Tang, Dong; Wu, Ping; Meng, Xu; Chen, Baohua published the artcile< Copper-catalyzed oxidative coupling reaction of α,β-unsaturated aldehydes with amidines: synthesis of 1,2,4-trisubstituted-1H-imidazole-5-carbaldehydes>, Category: bromides-buliding-blocks, the main research area is aldehyde amidine oxidative coupling reaction; imidazole carbaldehyde preparation.

Practical and highly functional group-compatible synthesis of 1,2,4-trisubstituted-1H-imidazole-5-carbaldehydes were developed via copper-catalyzed oxidative coupling of amidines and α,β-unsaturated aldehydes, which features aldehyde preservation, cheap catalysts, as well as high atom economy and mild conditions.

Organic Chemistry Frontiers published new progress about Amidines Role: RCT (Reactant), RACT (Reactant or Reagent). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cody, John; Fahrni, Christoph J. published the artcile< Fluorescence sensing based on cation-induced conformational switching: copper-selective modulation of the photoinduced intramolecular charge transfer of a donor-acceptor biphenyl fluorophore>, Recommanded Product: 4-Bromo-3-formylbenzonitrile, the main research area is fluorescence sensing cation induced conformational switching copper selective modulation; photoinduced intramol charge transfer donor acceptor biphenyl fluorophore.

The fluorescence emission energy of donor-acceptor substituted biphenyls is highly sensitive towards conformational changes of the interannular twist angle. By integrating 4-dimethylamino-4′-cyano-biphenyl into the ligand backbone of a thioether-rich metal receptor we designed a fluorescence sensor that exhibits high selectivity towards copper. Upon metal binding the ligand undergoes a significant conformational change, which induces a strong hypsochromic shift of the photoinduced charge-transfer emission. Steady-state absorption and fluorescence spectroscopy revealed a high affinity towards Cu(I) with a well-defined 1:1 metal-ligand complex stoichiometry. The nature of the conformational changes upon Cu(I) coordination were analyzed in detail by 1H NMR and 2D NOESY experiments The spectroscopic data provide a coherent picture, which is consistent with a Boltzmann ground-state distribution of several rotamers that are locked into a more flattened geometry upon coordination of Cu(I).

Tetrahedron published new progress about Fluorescence spectroscopy. 89003-95-2 belongs to class bromides-buliding-blocks, and the molecular formula is C8H4BrNO, Recommanded Product: 4-Bromo-3-formylbenzonitrile.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Da, Ya-jing; Yuan, Wei-dong; Xin, Ting; Nie, Yong-yan; Ye, Ying; Yan, Yi-Jia; Liang, Li-sha; Chen, Zhi-long published the artcile< Synthesis and biological evaluation of new fluorine substituted derivatives as angiotensin II receptor antagonists with anti-hypertension and anti-tumor effects>, Category: bromides-buliding-blocks, the main research area is fluorine compound preparation angiotensin II receptor antagonist SAR; antihypertensive antitumor losartan fluorinated derivative preparation SAR.

The synthesis and pharmaceutical activity of new potent non-tetrazole angiotensin II (Ang II) receptor antagonists were described. These compounds were fluorine substituted derivatives of Losartan, Valsartan and Irbesartan with carboxylic acid group as replacements to the known potent tetrazole moiety at the 2′-biphenyl position. Their activities were evaluated by Ang II receptor binding assay as well as by in vivo assay. All of the synthesized compounds showed nanomolar affinity for the AT1 receptor subtype. The vivo biol. evaluation showed that compounds 1a, 2 and 4 (I) produced a dose-dependent antihypertensive effect both in spontaneously hypertensive rats (SHR) and renal hypertensive rats (RHR). Compound 4 especially showed an efficient and long-lasting effect in reducing blood pressure which can last more than 24 h at dose of 10 mg/kg in SHR, which was much better than control Losartan and Valsartan. Compound 4 can also inhibit the prostate cancer in vitro and in vivo. So compound 4 was selected for in-depth investigation as potent, novel and long-lasting non-tetrazole anti-hypertension and anti-tumor drug candidate.

Bioorganic & Medicinal Chemistry published new progress about Angiotensin II receptor antagonists. 6942-39-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H6BrFO2, Category: bromides-buliding-blocks.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hanafi, Maha; Chen, Xinde; Neamati, Nouri published the artcile< Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91>, Recommanded Product: 4-Bromoisobenzofuran-1,3-dione, the main research area is tumorigenesis oncogenic pathways PROTACs STAT3 E3 ligase cytotoxicity degrader.

Napabucasin, undergoing multiple clin. trials, was reported to inhibit the signal transducer and transcription factor 3 (STAT3). To better elucidate its mechanism of action, we designed a napabucasin-based proteolysis targeting chimera (PROTAC), XD2-149(I) that resulted in inhibition of STAT3 signaling in pancreatic cancer cell lines without inducing proteasome-dependent degradation of STAT3. Proteomics anal. of XD2-149 revealed the downregulation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 degrades ZFP91 with DC50 values in the nanomolar range. The cytotoxicity of XD2-149 was significantly, but not fully, reduced with ZFP91 knockdown providing evidence for its multi-targeted mechanism of action. The NQO1 inhibitor, dicoumarol, rescued the cytotoxicity of XD2-149 but not ZFP91 degradation, suggesting that the NQO1-induced cell death is independent of ZFP91. ZFP91 plays a role in tumorigenesis and is involved in multiple oncogenic pathways including NF-κB and HIF-1α.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Recommanded Product: 4-Bromoisobenzofuran-1,3-dione.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tanimoto, Kouichi; Nakagawa, Naomichi; Takeda, Kazutaka; Kirihata, Mitsunori; Tanimori, Shinji published the artcile< A convenient one-pot access to phenanthridinones via Suzuki-Miyaura cross-coupling reaction>, Product Details of C8H6BrFO2, the main research area is phenanthridinone preparation Suzuki Miyaura coupling aminophenylboronic acid halobenzoate.

A convenient one-step access to biol. important phenanthridinones has been realized based upon Suzuki-Miyaura cross-coupling reaction. Reactions of 2-aminophenylboronic acid with 2-halobenzoate took place smoothly to afford substituted phenanthridinones in excellent yields in the presence of palladium(II) acetate and 2-dicyclohexylphosphino-2′,6′-dimethoxybiphenyl (SPhos) as pre-catalysts. A natural product phenaglydon was synthesized in one-pot manner from readily available starting materials in 95% yield.

Tetrahedron Letters published new progress about Aromatic carboxylic acids, esters Role: RCT (Reactant), RACT (Reactant or Reagent). 6942-39-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H6BrFO2, Product Details of C8H6BrFO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary