Tag: M.W=200-250

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, 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

Karad, Somnath Narayan published the artcileEnantioselective Synthesis of Chiral Cyclopent-2-enones by Nickel-Catalyzed Desymmetrization of Malonate Esters, Recommanded Product: 3-Chloro-4-isopropoxyphenylboronic acid, the main research area is chiral cyclopentenone enantioselective synthesis; crystal mol structure phenyl cyclopentenone; nickel catalyzed desymmetrization alkynyl malonate ester arylboronic acid; asymmetric catalysis; carbocycles; cyclization; isomerization; nickel.

The enantioselective synthesis of highly functionalized chiral cyclopent-2-enones by the reaction of alkynyl malonate esters with arylboronic acids is described. These desymmetrizing arylative cyclizations are catalyzed by a chiral phosphinooxazoline/nickel complex, and cyclization is enabled by the reversible E/Z isomerization of alkenylnickel species. The general methodol. is also applicable to the synthesis of 1,6-dihydropyridin-3(2H)-ones.

Angewandte Chemie, International Edition published new progress about Arylboronic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Recommanded Product: 3-Chloro-4-isopropoxyphenylboronic acid.

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

Xu, Liang published the artcileOxidative cyclization of N-alkyl-o-methyl-arenesulfonamides to biologically important saccharin derivatives, HPLC of Formula: 7079-48-3, the main research area is ortho methylarenesulfonamide oxidative cyclization saccharin derivative synthesis; benzisothiazole dioxide synthesis oxidative cyclization ortho methylarenesulfonamide.

Various biol. important saccharin skeletons and their N-alkyl derivatives were efficiently prepared by Cr(VI) oxide-catalyzed H5IO6 oxidation of N-alkyl-o-methyl-arenesulfonamides in MeCN. N-tert-Bu saccharin skeletons were easily prepared by H5IO6-CrO3 oxidation of N-tert-butyl-o-Me arenesulfonamides in the presence of acetic anhydride. The method that furnished the novel fluoro- and trifluoromethyl-substituted saccharin skeletons was characterized by two steps, a simple work-up procedure, a single purification and good overall yields from substituted toluene derivatives For example, 58 % 2-tert-butyl-6-trifluoromethyl-1,2-benzisothiazol-3-one 1,1-dioxide was obtained from 1-methyl-4-(trifluoromethyl)benzene.

Tetrahedron published new progress about Heterocyclization (oxidative). 7079-48-3 belongs to class chlorides-buliding-blocks, name is 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, and the molecular formula is C7H6ClFO2S, HPLC of Formula: 7079-48-3.

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

Spicer, Julie A. published the artcileSubstituted arylsulphonamides as inhibitors of perforin-mediated lysis, Name: 4-Fluoro-2-methylbenzene-1-sulfonyl chloride, the main research area is arylsulfonamide perforin mediated lysis inhibitor structure activity Immunosuppressive; Arylsulphonamide; Bioisostere; Immunosuppressant; Perforin; Perforin inhibitor.

The structure-activity relationships for a series of arylsulfonamide-based inhibitors of the pore-forming protein perforin have been explored. Perforin is a key component of the human immune response, however, inappropriate activity has also been implicated in certain auto-immune and therapy-induced conditions such as allograft rejection and graft vs. host disease. Since perforin is expressed exclusively by cells of the immune system, inhibition of this protein would be a highly selective strategy for the immunosuppressive treatment of these disorders. Compounds from this series were demonstrated to be potent inhibitors of the lytic action of both isolated recombinant perforin and perforin secreted by natural killer cells in vitro. Several potent and soluble examples were assessed for in vivo pharmacokinetic properties and found to be suitable for progression to an in vivo model of transplant rejection.

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

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