Tag: M.W=200-250

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

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

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

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

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

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

Yu, Bin; Zhao, Bin; Hao, Zesheng; Chen, Lei; Cao, Lixin; Guo, Xiaofeng; Zhang, Nailou; Yang, Dongyan; Tang, Liangfu; Fan, Zhijin published the artcile< Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors>, Related Products of 5751-83-7, the main research area is pyrazole thiazole aryl carboxamide preparation antifungal SDH inhibitor SAR; Antifungal activity; Molecular docking; Structure-activity relationships; Succinate dehydrogenase inhibitors.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

European Journal of Medicinal Chemistry published new progress about Amides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Related Products of 5751-83-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Sha; Zhou, Shaa; Xie, Yong-Tao; Jin, Ru-Yi; Meng, Xiang-De; Zhang, Dong-Kai; Hua, Xue-Wen; Liu, Ming; Wu, Chang-Chun; Xiong, Li-Xia; Zhao, Yu; Li, Zheng-Ming published the artcile< The exploration of chiral N-cyano sulfiliminyl dicarboxamides on insecticidal activities>, Computed Properties of 82-73-5, the main research area is chiral cyano sulfiliminyl dicarboxamide preparation insecticide Pseudaletia larva.

Due to new mechanism of action and ecofriendly characteristics, dicarboxamide insecticides have attracted more and more attentions in modern pest management. A series of 20 dual chiral N-cyano sulfilimines containing two centers (carbon and sulfur) were designed and synthesized. All title compounds were determined by 1H NMR, high-resolution mass spectrometry (HRMS) and optical polarimeter. The preliminary results indicated that some of them exhibited favorable insecticidal activities against oriental armyworm (Pseudaletia separata Walker). These isomers exhibited different impact on activity following the sequence as (Sc, Ss) ≥ (Sc, Rs), and the rule of title compounds’ activity against oriental armyworm was 3-CF3 ≥ 2-CH3-4-Cl >2, 3, 4-trifluro in the anilide moiety. The results indicated that these groups such as 3-CF3, 2-CH3-4-Cl or 2, 3, 4-trifluro were inefficient to replace heptafluoroisopropyl group for high larvicidal activity, which provided some guidance for the further modifications of sulfiliminyl dicarboxamides.

Chinese Chemical Letters published new progress about Insecticides. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Computed Properties of 82-73-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Genov, Georgi R.; Douthwaite, James L.; Lahdenpera, Antti S. K.; Gibson, David C.; Phipps, Robert J. published the artcile< Enantioselective remote C-H activation directed by a chiral cation>, Safety of 3-Bromobenzotrifluoride, the main research area is benzhydrylamide phoshinamide enantioselective borylation remote bond activation chiral cation.

Chiral cations have been used extensively as organocatalysts, but their application to rendering transition metal-catalyzed processes enantioselective remains rare. This is despite the success of the analogous charge-inverted strategy in which cationic metal complexes are paired with chiral anions. We report here a strategy to render a common bipyridine ligand anionic and pair its iridium complexes with a chiral cation derived from quinine. We have applied these ion-paired complexes to long-range asym. induction in the desymmetrization of the geminal diaryl motif, located on a carbon or phosphorus center, by enantioselective C-H borylation. In principle, numerous common classes of ligand could likewise be amenable to this approach.

Science (Washington, DC, United States) published new progress about Absolute configuration. 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Safety of 3-Bromobenzotrifluoride.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Zhenghong; Hu, Kangfei; Wang, Jiawei; Li, Zhibin; Zhang, Yan; Zha, Zhenggen; Wang, Zhiyong published the artcile< Electrosynthesis of Quinazolines and Quinazolinones via an Anodic Direct Oxidation C(sp3)-H Amination/C-N Cleavage of Tertiary Amine in Aqueous Medium>, Application of C7H6BrNO, the main research area is quinazoline quinazolinone electrochem preparation green chem; tertiary amine carbonyl aniline anodic oxidation amination cleavage.

An electrochem. synthesis for quinazolines and quinazolinones was developed via a C(sp3)-H amination/C-N cleavage by virtue of the anodic oxidation The reaction can be carried out in aqueous media under mild conditions to afford the desired products with high yields. The reaction mechanism was proposed after detailed investigation.

ACS Omega published new progress about Amination. 29124-57-0 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO, Application of C7H6BrNO.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary