Category: chlorides-buliding-blocks

Cho, Sung Jin published the artcileSelective 5-Hydroxytryptamine 2C Receptor Agonists Derived from the Lead Compound Tranylcypromine: Identification of Drugs with Antidepressant-Like Action, Formula: C8H6ClFO, the main research area is serotonin receptor 5HT2c agonist antidepressant tranylcypromine derivative SAR preparation.

We report here the design, synthesis, and pharmacol. properties of a series of compounds related to tranylcypromine (9), which itself was discovered as a lead compound in a high-throughput screening campaign. Starting from 9, which shows modest activity as a 5-HT2C agonist, a series of 1-aminomethyl-2-phenylcyclopropanes was investigated as 5-HT2C agonists through iterative structural modifications. Key pharmacophore feature of this new class of ligands is a 2-aminomethyl-trans-cyclopropyl side chain attached to a substituted benzene ring. Among the tested compounds, several were potent and efficacious 5-HT2C receptor agonists with selectivity over both 5-HT2A and 5-HT2B receptors in functional assays. The most promising compound is 37, with 120- and 14-fold selectivity over 5-HT2A and 5-HT2B, resp. (EC50 = 585, 65, and 4.8 nM at the 2A, 2B, and 2C subtypes, resp.). In animal studies, compound 37 (10-60 mg/kg) decreased immobility time in the mouse forced swim test.

Journal of Medicinal Chemistry published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Formula: C8H6ClFO.

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

Kas’yan, L. I. published the artcile2-(1-Aminoethyl)bicyclo[2.2.1]heptane. Sulfonamides, ureas, and thioreas on its base, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is aminoethylbicycloheptane conformation electron density nucleophilic reactivity; sulfonamide aminoethylbicycloheptane preparation; urea aminoethylbicycloheptane preparation; thiourea aminoethylbicycloheptane preparation.

The known antiviral drug, 2-(1-aminoethyl)bicyclo[2.2.1]heptane, has been studied by mol. mechanics and quantum-chem. methods. The structure of both exo and endo isomers has been examined by the MMX procedure. Conformational compositions of the isomers and barriers to rotation about the C2-C8 bond have been compared with corresponding parameters of stereoisomeric 2-aminomethylbicyclo[2.2.1]heptanes which also exhibit antiviral activity. The electron d. distribution in the amines has been calculated by the semiempirical AM1 method, and their reactivity has been estimated on the basis of the calculated proton affinities and energies of localized MOs. Nucleophilic properties of the title compound have been studied in reactions with phenylmethane- and arenesulfonyl chlorides and alicyclic and aromatic isocyanates and isothiocyanates. The structure of sulfonamides, ureas, and thioureas thus obtained has been proved by IR and 1H spectroscopy.

Russian Journal of Organic Chemistry (Translation of Zhurnal Organicheskoi Khimii) published new progress about Amines Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent) (cage). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Recommanded Product: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride.

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

Toyota, Kozo published the artcileUnexpected formation of 4,7-dihalobenzo[b]thiophenes using Ohira-Bestmann reagent and reactivity of the halogen-substituted benzo[b]thiophenes in Suzuki-Miyaura coupling with phenylboronic acid, HPLC of Formula: 886615-30-1, the main research area is phenyl halobenzothiophene preparation regioselective; phenylboronic acid dihalobenzothiophene Suzuki coupling palladium catalyst.

Reaction of 2-(1-adamantylsulfanyl)-3,6-dihalobenzaldehydes 2-X-5-Y-6-SR1C6H2CHO (X = Br, I, Cl, H, Ph; Y = Br, I, Cl, H; R1 = adamantan-1-yl) with Ohira-Bestmann reagent gave 4,7-dihalobenzo[b]thiophenes I along with normal alkyne products 2-X-5-Y-6-SR1C6H2CC . Nine types of 4,7-dihalobenzo[b]thiophenes I bearing chlorine, bromine, or iodine atoms, were prepared by this method. Regioselectivity in Suzuki-Miyaura cross coupling reactions of the 4,7-dihalobenzo[b]thiophenes I with PhB(OH)2 was also studied.

Heterocycles published new progress about Aromatic hydrocarbons, aryl alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 886615-30-1 belongs to class chlorides-buliding-blocks, name is 3-Bromo-6-chloro-2-fluorobenzaldehyde, and the molecular formula is C7H3BrClFO, HPLC of Formula: 886615-30-1.

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

Kim, Ikyon published the artcileDesign, synthesis, and evaluation of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors, Recommanded Product: Ethyl 2,5-dichlorobenzoate, the main research area is aryldialkoxyphenylpyrazolopyrimidine preparation PDE4 inhibitor.

Described herein is design, synthesis, and biol. evaluation of novel series of 2-aryl-7-(3′,4′-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines acting as inhibitors of type 4 phosphodiesterase (PDE4) which is known as a good target for the treatment of asthma and COPD. For this purpose, structure optimization was conducted with the aid of structure-based drug design using the known X-ray crystallog. Also, biol. effects of these compounds on the target enzyme were evaluated by using in vitro assays, leading to the potent and selective PDE-4 inhibitor (IC50 < 10 nM). Bioorganic & Medicinal Chemistry Letters published new progress about Asthma. 35112-27-7 belongs to class chlorides-buliding-blocks, name is Ethyl 2,5-dichlorobenzoate, and the molecular formula is C9H8Cl2O2, Recommanded Product: Ethyl 2,5-dichlorobenzoate.

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

Mikami, Shinichi published the artcileSilica gel-assisted preparation of 2,4,7-trihalobenzo[b]thiophenes and 4,7-dihalobenzo[b]thiophenes, Recommanded Product: 3-Bromo-6-chloro-2-fluorobenzaldehyde, the main research area is halobenzothiophene preparation.

All 6 isomers of (bromo)(chloro)(iodo)benzo[b]thiophenes containing three different halogen atoms at the 2-, 4- and 7-positions I (X = I, Br, Cl; Y = I, Br, Cl; Z = I, Br, Cl) were synthesized from the corresponding 2-(1-adamantylsulfanyl)-1,4-dihalo-3-(haloethynyl)benzene derivatives 2-RS-3-ZCC-4-XC6H2Y (R = adamantan-1-yl), through treatment with silica gel under thermal conditions. In contrast to the previous method using gold chloride catalyst, migration of adamantyl group did not occur in this method using silica gel. Moreover, by using this method, 6 types of 4,7-dihalobenzo[b]thiophenes I (Z = H) have been synthesized in 4 steps from 2-fluoro-3,6-dihalo-benzaldehydes 2-F-3Y-6-XC6H2CHO in moderate to excellent overall yields (42-82%).

Phosphorus, Sulfur and Silicon and the Related Elements published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 886615-30-1 belongs to class chlorides-buliding-blocks, name is 3-Bromo-6-chloro-2-fluorobenzaldehyde, and the molecular formula is C7H3BrClFO, Recommanded Product: 3-Bromo-6-chloro-2-fluorobenzaldehyde.

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

Mikami, Shinichi published the artcileSilica gel-assisted preparation of (bromo)(chloro)(iodo)benzo[b]thiophenes bearing halogen atoms at the 2-, 4-, and 7-positions, Name: 4-Chloro-2-fluoroiodobenzene, the main research area is benzothiophene dihalo trihalo preparation stereoselective silica gel; sulfide adamantyl alkynylaryl halo preparation intramol cyclization silica.

Six types of (bromo)(chloro)(iodo)benzo[b]thiophenes bearing halogen atoms at the 2-, 4-, and 7-positions were prepared from the corresponding 2-(1-adamantylthio)-1,4-dihalo-3-(haloethynyl)benzene derivatives, by treatment with silica gel under thermal conditions. 4,7-Dihalobenzo[b]thiophenes, bearing two different halogen atoms (chlorine, bromine, or iodine), were also prepared from 2-(1-adamantylthio)-3-(ethynyl)-1,4-dihalobenzenes.

Heterocycles published new progress about Aldehydes, halo Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6797-79-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoroiodobenzene, and the molecular formula is C6H3ClFI, Name: 4-Chloro-2-fluoroiodobenzene.

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

Mikami, Shinichi published the artcileSilica gel-assisted preparation of (bromo)(chloro)(iodo)benzo[b]thiophenes bearing halogen atoms at the 2-, 4-, and 7-positions, Product Details of C7H3BrClFO, the main research area is benzothiophene dihalo trihalo preparation stereoselective silica gel; sulfide adamantyl alkynylaryl halo preparation intramol cyclization silica.

Six types of (bromo)(chloro)(iodo)benzo[b]thiophenes bearing halogen atoms at the 2-, 4-, and 7-positions were prepared from the corresponding 2-(1-adamantylthio)-1,4-dihalo-3-(haloethynyl)benzene derivatives, by treatment with silica gel under thermal conditions. 4,7-Dihalobenzo[b]thiophenes, bearing two different halogen atoms (chlorine, bromine, or iodine), were also prepared from 2-(1-adamantylthio)-3-(ethynyl)-1,4-dihalobenzenes.

Heterocycles published new progress about Aldehydes, halo Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 886615-30-1 belongs to class chlorides-buliding-blocks, name is 3-Bromo-6-chloro-2-fluorobenzaldehyde, and the molecular formula is C7H3BrClFO, Product Details of C7H3BrClFO.

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

Szupiluk, Artur published the artcileSynthesis of sterically crowded 9-nitrotriptycenes by the Diels-Alder cycloaddition reaction, SDS of cas: 3032-32-4, the main research area is nitroanthracene halobenzyne regioselective Diels Alder reaction; nitrotriptycene preparation.

The synthesis of novel sterically crowded triptycenes as attractive components for the construction of models for various mol. dynamic studies was reported. 9-Nitrotriptycenes were obtained by the Diels-Alder reactions between 9-nitroanthracene and tetrabromobenzyne as well as 1,4-dichloro-9-nitroanthracene and 2,6-dichlorobenzyne. Interesting regioselectivity relative to the central and terminal rings was observed Moreover, 1,2,3,4-tetrabromo-9-nitrotriptycene was further functionalized to afford 1,2,3,4-tetrabromotriptycyl-9-ammonium tetrafluoroborate in two-steps. The impact of steric hindrance on the geometry of the mol. was estimated on the basis of single crystal X-ray diffraction data.

Tetrahedron Letters published new progress about Diels-Alder reaction, regioselective. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, SDS of cas: 3032-32-4.

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

Pal, Manojit published the artcileSynthesis and Cyclooxygenase-2 Inhibiting Property of 1,5-Diarylpyrazoles with Substituted Benzenesulfonamide Moiety as Pharmacophore: Preparation of Sodium Salt for Injectable Formulation, Category: chlorides-buliding-blocks, the main research area is diarylpyrazole containing benzenesulfonamide pharmacophore preparation cyclooxygenase 2 inhibitor; sulfamoylphenylpyrazole preparation cyclooxygenase 2 inhibitor; pyrazolylbenzenesulfonamide preparation cyclooxygenase 2 inhibitor.

A series of 1,5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore, e.g. (I; Ar = 2 or 3-fluoro-4-sulfamoylphenyl, 3-methyl-4-sulfamoylphenyl; R = OMe, SMe) and (II; R1 = 4-methoxyphenyl, 4-methylthiophenyl, 4-fluorophenyl; R2= propanoyl, butyryl) was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Through SAR and mol. modeling, it was found that fluorine substitution on the benzenesulfonamide moiety along with an electron-donating group at the 4-position of the 5-aryl ring yielded selectivity as well as potency for COX-2 inhibition in vitro. Among such compounds 3-fluoro-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide 3 displayed interesting pharmacokinetic properties along with antiinflammatory activity in vivo. Among the sodium salts tested in vivo, 10, the propionyl analog of 3, showed excellent antiinflammatory activity and therefore represents a new lead structure for the development of injectable COX-2 specific inhibitors.

Journal of Medicinal Chemistry published new progress about Pharmacokinetics. 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, Category: chlorides-buliding-blocks.

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

Saha, Debasmita published the artcileFacile Construction of Imidazo-benzothia-/oxazepines by a Quick and Efficient van Leusen Protocol, Recommanded Product: 2-Chloro-3-(trifluoromethyl)benzaldehyde, the main research area is dihydrodibenzoimidazothiazepine preparation; isocyanide dibenzothiazepine preparation Van Leusen; dihydrodibenzoimidazooxazepine preparation; dibenzoxazepine preparation isocyanide Van Leusen protocol.

A facile, elegant, and operationally simple Van Leusen protocol for the synthesis of bicyclic dihydrodibenzo[b,f]imidazo[1,2-d][1,4]thiazepines I [X = S; R1 = R2 = R4 = H, Cl; R3 = H, NO2; R5 = C(O)OEt, Ts] and dihydrodibenzo[b,f]imidazo[1,2-d][1,4]oxazepines I [X = O] was developed. The reaction proceeded without any catalyst and in high yields to provide bicyclic imidazo-dibenzothia-/oxazepines at room temperature by using dibenzothiazepines or dibenzoxazepines as imine counterparts.

Asian Journal of Organic Chemistry published new progress about Benzaldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Recommanded Product: 2-Chloro-3-(trifluoromethyl)benzaldehyde.

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