Tag: M.W=200-250

Chang, Ning-hui published the artcileSynthesis of Substituted Picenes through Pd-Catalyzed Cross-Coupling Reaction/Annulation Sequences and Their Physicochemical Properties, Application In Synthesis of 3032-32-4, the main research area is picene chemoselective preparation; palladium catalyzed Suzuki Miyaura coupling cyclocondensation chloroiodobenzene aralkenylboronate; methoxypicene preparation mol crystal structure.

Picenes I (R = H, Et; R1 = H, MeO; R2 = H, Me3Si; R3 = H, MeO; R4 = H, MeO) were prepared from 1,4-dichloro-2,3-diiodobenzene and alkenyl pinacolboronates II (R = H, Et; R1 = H, MeO; R2 = H, Me3Si; R3 = H, MeO; R4 = H, MeO; BPin = 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) by palladium-catalyzed Suzuki-Miyaura coupling to give 2,3-bis(arylalkenyl)-1,4-dichlorobenzenes III (R = H, Et; R1 = H, MeO; R2 = H, Me3Si; R3 = H, MeO; R4 = H, MeO) in 38-68% yields followed by palladium-catalyzed cyclization and C-H activation to give I in 23-60% yields. The UV/visible absorption and fluorescence spectra, HOMO and LUMO energies and orbital structures, and oxidation potentials for I were determined; I were p-type semiconductors and were stable to cyclic voltammetry. The structure of I (R = R1 = R2 = R3 = H; R4 = MeO) was determined by X-ray crystallog.

Organic Letters published new progress about C-H bond activation. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Application In Synthesis of 3032-32-4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Marivingt-Mounir, Cecile published the artcileSynthesis, SAR, Crystal Structure, and Biological Evaluation of Benzoquinoliziniums as Activators of Wild-Type and Mutant Cystic Fibrosis Transmembrane Conductance Regulator Channels, COA of Formula: C9H8Cl2O2, the main research area is benzoquinolizinium preparation cystic fibrosis transmembrane conductance regulator channel activation; benzoindoloquinolizinium preparation cystic fibrosis transmembrane conductance regulator channel activation.

Chloride channels play important roles in homeostasis and regulate cell volume, transepithelial transport, and elec. excitability. Despite recent progress made in the genetic and mol. aspect of chloride channels, their pharmacol. is still poorly understood. The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated epithelial chloride channel for which mutations cause cystic fibrosis. Here we have synthesized benzo[c]quinolizinium, e.g., I, and benzo[f]indolo[2,3-a]quinolizinium salts (MPB), e.g., II, and performed a SAR to identify the structural basis for activation of the CFTR chloride channel. Synthesized compounds were evaluated on wild-type CFTR and on CFTR having the glycine-to-aspartic acid missense mutation at codon 551 (G551D-CFTR), using a robot and cell-based assay. The presence of an hydroxyl group at position 6 of the benzo[c]quinolizinium skeleton associated with a chlorine atom at position 10 or 7 and an alkyl chain at position 5 determined the highest activity. The most potent product is 5-butyl-7-chloro-6-hydroxybenzo[c]quinolizinium chloride (I, MPB-104). I is 100 times more potent than the parent compound III (MPB-07).

Journal of Medicinal Chemistry published new progress about Chloride channels Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, COA of Formula: C9H8Cl2O2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jiang, Fei published the artcileDiscovery of Benzo[cd]indol-2(1H)-ones and Pyrrolo[4,3,2-de]quinolin-2(1H)-ones as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain with Potential High Efficiency against Acute Gouty Arthritis, Related Products of chlorides-buliding-blocks, the main research area is preparation benzoindolone pyrrolo quinolinone derivative BET inhibitor gout.

The bromodomain and extra-terminal domain (BET) family of proteins are readers which specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein contains two highly homologous domains: the first bromodomain (BD1) and the second bromodomain (BD2). Pan-BET bromodomain inhibition is a potential therapy for various cancers and immune-inflammatory diseases, but only few reported inhibitors show selectivity within the BET family. Herein, we identified a series of benzo[cd]indol-2(1H)-ones and pyrrolo[4,3,2-de]quinolin-2(1H)-ones with good selectivity for BET BD1. Through structure-based optimization, highly active and selective compounds are ultimately obtained. The representative compounds are the first reported inhibitors with selectivity more than 100-fold for BRD4(1) over BRD4(2). Among them, we further show that 68 (LT052) mediates BRD4/NF-κB/NLRP3 signaling inflammatory pathways with comparable protein expression and significantly improves symptoms of gout arthritis in a rat model. Therefore, selective pharmacol. modulation of individual bromodomains could represent a strategy for the treatment of acute gouty arthritis.

Journal of Medicinal Chemistry published new progress about Bromodomain-containing protein BRD4 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Related Products of chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Fadeeva, Anastasia A. published the artcileChlorination of Conjugated Nitroalkenes with PhICl2 and SO2 Cl2 for the Synthesis of α-Chloronitroalkenes, Computed Properties of 61343-99-5, the main research area is conjugated nitroalkene iodobenzene dichloride chemoselective chlorination; sulfuryl chloride conjugated nitroalkene chemoselective chlorination; chloro nitroalkene preparation.

Chlorination of conjugated nitroalkenes with iodobenzene dichloride or sulfuryl chloride to give target α-chloronitroalkenes in good yields was described. Details of the procedure depend on the donating ability of the nitroalkene substituents. The activity of the described chlorinating agents increases in order ‘PhICl2/Py’ < 'SO2Cl2' < 'SO2Cl2/HCl' with the former produced the best yields for highly donating substrates and the latter for non-activated groups. An autocatalytic role of hydrogen chloride and the chemoselectivity of chlorination were also demonstrated. Synthesis published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 61343-99-5 belongs to class chlorides-buliding-blocks, name is 4-(4-Chlorophenoxy)benzaldehyde, and the molecular formula is C13H9ClO2, Computed Properties of 61343-99-5.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Li, Jian-Yuan; Miklossy, Gabriella; Modukuri, Ram K.; Bohren, Kurt M.; Yu, Zhifeng; Palaniappan, Murugesan; Faver, John C.; Riehle, Kevin; Matzuk, Martin M.; Simmons, Nicholas published the artcile< Palladium-Catalyzed Hydroxycarbonylation of (Hetero)aryl Halides for DNA-Encoded Chemical Library Synthesis>, Reference of 2382-10-7, the main research area is palladium catalyzed hydroxycarbonylation heteroaryl halide DNA encoded library synthesis.

A strategy for DNA-compatible, palladium-catalyzed hydroxycarbonylation of (hetero)aryl halides on DNA-chem. conjugates has been developed. This method generally provided the corresponding carboxylic acids in moderate to very good conversions for (hetero)aryl iodides and bromides, and in poor to moderate conversions for (hetero)aryl chlorides. These conditions were further validated by application within a DNA-encoded chem. library synthesis and subsequent discovery of enriched features from the library in selection experiments against two protein targets.

Bioconjugate Chemistry published new progress about Carbonylation. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Reference of 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhou, Guanyu; Huang, Zhibin; Xu, Xu; Fang, Zhang; Huang, Pengcheng; Deng, Zefeng; Li, Bao; Zhao, Yingsheng published the artcile< Rhodium(III)-Catalyzed Synthesis of Quinazolin-4(3H)-ones with N-Methoxyamides as Synthesis Reagents>, Related Products of 162046-61-9, the main research area is methoxy aryl quinazolinone preparation.

A practical method to synthesize quinoxalinones I [R = H, 6-Me, 7-Et, etc.; R1 = H, 3-Br, 3-MeO, etc.] via intra/intermol. amination using rhodium as the catalyst was developed. A wide variety of quinoxalinones I were prepared from N-methoxybenzamides in moderate to excellent yields. Gram-scale reactions were also achieved, highlighting the synthetic importance of this new transformation.

Synthesis published new progress about Amination. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Related Products of 162046-61-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Martins, Solange C.; Desoti, Vania C.; Lazarin-Bidoia, Danielle; Vandresen, Fabio; da Silva, Cleuza C.; Ueda-Nakamura, Tania; Silva, Sueli de O.; Nakamura, Celso V. published the artcile< Synthesis and evaluation of the trypanocidal activity of a series of 1,3,4-thiadiazole derivatives of R-(+)-limonene benzaldehyde-thiosemicarbazones>, Related Products of 70057-67-9, the main research area is thiadiazole preparation trypanocidal cytotoxicity.

A series of 1,3,4-thiadiazole derivatives of R-(+)-limonene benzaldehyde-thiosemicarbazones I has been synthesized. The synthesized compounds and a series of 1,3,4-thiadiazole without the monoterpene R-(+)-limonene II were tested in in-vitro assays against epimastigote and trypomastigote forms of T. cruzi, and the cytotoxicity was also determined in LLCMK2 cells. The 1,3,4-thiadiazole compounds showed significant trypanocidal activity and a high selectivity indexes. The vast majority of the monoterpene derivatives, substituted by R-(+)-limonene, presented better anti-T. cruzi activity than the non-substituted compounds Regarding the cytotoxic profile, the compounds without the monoterpene R-(+)-limonene were, in general, less toxic. The present findings indicate that the 1,3,4-thiadiazoles derivatives of R-limonene have potential trypanocidal activity that justify further studies to better understand the mechanism of action of these substances on T. cruzi.

Medicinal Chemistry Research published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Related Products of 70057-67-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zhao, Zhigang; Li, Lin; Liu, Min; Mei, Qinggang published the artcile< An efficient synthesis of novel bis-1,3,4-thiadiazolyl-carbamate derivatives based on deoxycholic acid under microwave irradiation>, Category: chlorides-buliding-blocks, the main research area is carboxylate thiosemicarbazide cyclocondensation; thiadiazole amine preparation carbamation deoxycholate; thiadiazolyl carbamate cholanoate preparation microwave.

An easy and efficient method for the synthesis of novel deoxycholic acid bis-1,3,4-thiadiazol-carbamate derivatives under microwave irradiation was developed. Twelve new Me 3α,12α-bis-[(5-aryl-1,3,4-thiadiazol-2-yl)carbamoyloxy]-cholan-24-oates were obtained in better yield (78-91%) and shorter time (15-22 min). Their structures were identified by 1H NMR, IR, MS spectra and elemental analyses.

Journal of Chemical Research published new progress about Aromatic carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jiao, Ke-Jin; Liu, Dong; Ma, Hong-Xing; Qiu, Hui; Fang, Ping; Mei, Tian-Sheng published the artcile< Nickel-Catalyzed Electrochemical Reductive Relay Cross-Coupling of Alkyl Halides to Aryl Halides>, HPLC of Formula: 16799-05-6, the main research area is nickel catalyst electrochem reductive relay coupling alkyl halide aryl; arenes; cross-coupling; electrochemistry; nickel; reaction mechanisms.

A highly regioselective Ni-catalyzed electrochem. reductive relay cross-coupling between an aryl halide and an alkyl halide was developed in an undivided cell. Various functional groups are tolerated under these mild reaction conditions, which provides an alternative approach for the synthesis of 1,1-diarylalkanes.

Angewandte Chemie, International Edition published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, HPLC of Formula: 16799-05-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jatav, Varsha; Mishra, Pradeep; Kashaw, Sushil; Stables, J. P. published the artcile< Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is thiadiazolylstyryl quinazolinone preparation anticonvulsant sedative hypnotic CNS depressant agent.

A series of novel 3-[5-substituted phenyl-1,3,4-thiadiazol-2-yl]-2-styryl quinazoline-4(3H)-ones were synthesized and evaluated for anticonvulsant, sedative-hypnotic and CNS depressant activities. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight 2-styrylquinazolin-4(3H)-one derivatives were examined in the maximal electroshock induced seizures (MES) and s.c. pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. Out of eighteen compounds only five, e.g., I (R = H or Cl), showed anticonvulsant activity in one or more test models. All except two compounds exhibited significant sedative-hypnotic activity via actophotometer screen. CNS depressant activity screened with the help of the forced swim pool method resulted into some potent compounds From the exptl. observation it can be concluded that synthesized compounds exhibited relatively better sedative-hypnotic and CNS depressant activities.

European Journal of Medicinal Chemistry published new progress about Anticonvulsants. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics