Category: 53581-86-5

Gensini, Martina; Altamura, Maria; Dimoulas, Tula; Fedi, Valentina; Giannotti, Danilo; Giuliani, Sandro; Guidi, Antonio; Harmat, Nicholas J. S.; Meini, Stefania; Nannicini, Rossano; Pasqui, Franco; Tramontana, Manuela; Triolo, Antonio; Maggi, Carlo Alberto published the artcile< Modulation on C- and N-Terminal Moieties of a Series of Potent and Selective Linear Tachykinin NK2 Receptor Antagonists>, Name: 4-Chloro-2-methoxybenzaldehyde, the main research area is tachykinin NK2 receptor antagonist preparation structure activity.

Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the C- and N-terminal moieties of ibodutant (MEN 15596, 1). The N-terminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the mol. without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61 b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).

ChemMedChem published new progress about Colon (contractions). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Name: 4-Chloro-2-methoxybenzaldehyde.

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

Gensini, Martina; Altamura, Maria; Dimoulas, Tula; Fedi, Valentina; Giannotti, Danilo; Giuliani, Sandro; Guidi, Antonio; Harmat, Nicholas J. S.; Meini, Stefania; Nannicini, Rossano; Pasqui, Franco; Tramontana, Manuela; Triolo, Antonio; Maggi, Carlo Alberto published the artcile< Modulation on C- and N-Terminal Moieties of a Series of Potent and Selective Linear Tachykinin NK2 Receptor Antagonists>, Name: 4-Chloro-2-methoxybenzaldehyde, the main research area is tachykinin NK2 receptor antagonist preparation structure activity.

Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the C- and N-terminal moieties of ibodutant (MEN 15596, 1). The N-terminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the mol. without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61 b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).

ChemMedChem published new progress about Colon (contractions). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Name: 4-Chloro-2-methoxybenzaldehyde.

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

Bertrand, Sophie M.; Ancellin, Nicolas; Beaufils, Benjamin; Bingham, Ryan P.; Borthwick, Jennifer A.; Boullay, Anne-Benedicte; Boursier, Eric; Carter, Paul S.; Chung, Chun-wa; Churcher, Ian; Dodic, Nerina; Fouchet, Marie-Helene; Fournier, Charlene; Francis, Peter L.; Gummer, Laura A.; Herry, Kenny; Hobbs, Andrew; Hobbs, Clare I.; Homes, Paul; Jamieson, Craig; Nicodeme, Edwige; Pickett, Stephen D.; Reid, Iain H.; Simpson, Graham L.; Sloan, Lisa A.; Smith, Sarah E.; Somers, Donald O’N.; Spitzfaden, Claus; Suckling, Colin J.; Valko, Klara; Washio, Yoshiaki; Young, Robert J. published the artcile< The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits>, Name: 4-Chloro-2-methoxybenzaldehyde, the main research area is mitochondria aminotransferase inhibitor.

The hybridization of hits, identified by complementary fragment and high throughput screens, enabled the discovery of the first series of potent inhibitors of mitochondrial branched-chain aminotransferase (BCATm) based on a 2-benzylamino-pyrazolo[1,5-a]pyrimidinone-3-carbonitrile template. Structure-guided growth enabled rapid optimization of potency with maintenance of ligand efficiency, while the focus on physicochem. properties delivered compounds with excellent pharmacokinetic exposure that enabled a proof of concept experiment in mice. Oral administration of I significantly raised the circulating levels of the branched-chain amino acids leucine, isoleucine, and valine in this acute study.

Journal of Medicinal Chemistry published new progress about Crystal structure. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Name: 4-Chloro-2-methoxybenzaldehyde.

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

Ghosh, Santanu; Jana, Chandan K. published the artcile< Metal-Free Thermal Activation of Molecular Oxygen Enabled Direct α-CH2-Oxygenation of Free Amines>, HPLC of Formula: 53581-86-5, the main research area is thermal activation mol oxygen; alpha methylene oxygenation amine; amide lactam preparation.

Direct oxidation of α-CH2 group of free amines is hard to achieve due to the higher reactivity of amine moiety. Therefore, oxidation of amines involves the use of sophisticated metallic reagents/catalyst in the presence or absence of hazardous oxidants under sensitive reaction conditions. A novel method for direct C-H oxygenation of aliphatic amines through a metal-free activation of mol. oxygen has been developed. Both activated and unactivated free amines were oxygenated efficiently to provide a wide variety of amides (primary, secondary) and lactams under operationally simple conditions without the aid of metallic reagents and toxic oxidants. The method has been applied to the synthesis of highly functionalized amide-containing medicinal drugs, such as O-Me-alibendol and -buclosamide.

Journal of Organic Chemistry published new progress about Aliphatic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, HPLC of Formula: 53581-86-5.

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

Prasadarao, K.; Lusirani Susuma, A. J.; Mohan, S. published the artcile< Synthesis, characterization and antibacterial activity of few chalcones>, Electric Literature of 53581-86-5, the main research area is chlorohydroxyacetophenone aldehyde Claisen Schmidt condensation; chalcone preparation antibacterial.

A series of chalcones were synthesized by condensing 4-chloro-2-hydroxyacetophenone with aldehyde derivatives in dilute ethanolic sodium hydroxide solution at room temperature according to Claisen-Schmidt condensation. The synthesized compounds were characterized by means of their IR, 1H-NMR spectral data and elemental anal. All these compounds were tested for their antibacterial activity by agar well diffusion method.

International Journal of Pharma and Bio Sciences published new progress about Antibacterial agents. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Electric Literature of 53581-86-5.

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

Dubuffet, T.; Loutz, A.; Lavielle, G. published the artcile< An efficient large scale synthesis of coumarins by a dealkylative boron-mediated ring closure of 3-(ortho-methoxyaryl)propenoic esters>, HPLC of Formula: 53581-86-5, the main research area is coumarin synthesis; methoxyarylpropenoic ester preparation dealkylative boron mediated ring closure; methoxycinnamate ortho preparation dealkylative boron mediated ring closure.

Various substituted coumarins, e.g. I (R = H, 5-OH, 5-OMe, 6-OH, 8-OH, 6-Br, 7-Cl-6-Br, 6-Cl, 7-Cl, 8-Cl, 6-NO2, 7-F, 6-F), were prepared via a dealkylative boron-mediated ring closure of ortho-methoxycinnamates,e.g. II (R = H, 6-OMe, 5-OMe, 3-OMe, 5-Br, 5-Br-4-Cl, 5-Cl, 4-Cl, 3-Cl, 5-NO2, R1 = Me; R = 4-F, 5-F, R1 = Et).

Synthetic Communications published new progress about Cyclization (dealkylative). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, HPLC of Formula: 53581-86-5.

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

Gung, Benjamin W.; Smith, Daniel T.; Wolf, Mark A. published the artcile< Evidence for synclinal transition state in the reactions of aromatic aldehydes with α-(alkoxy)allylstannanes>, Synthetic Route of 53581-86-5, the main research area is aldehyde aromatic reaction alkoxyallylstannane stereochem; transition state structure aldehyde reaction alkoxyallylstannane; ether enol preparation stereoselective.

Unlike aliphatic aldehydes, aromatic aldehydes produce greater than 95% of syn-(Z)-enol ether when treated with α-(alkoxy)allylstannanes in the presence of BF3·Et2O. However, in the presence of TiCl4, the reaction of p-chloro-o-methoxybenzaldehyde with α-(alkoxy)crotylstannane produced predominantly the syn-(E) isomer.

Tetrahedron published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Synthetic Route of 53581-86-5.

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

Kumar, Balagani Sathish; Negi, Arvind S. published the artcile< A frank synthesis of alkyl-aryl ethers from 2-halobenzaldehydes and aromatic olefins without transition metal co-catalyst and ligand>, COA of Formula: C8H7ClO2, the main research area is alkyl aryl ether preparation halobenzaldehyde aromatic olefin.

An efficient synthesis of alkyl ethers was developed for o-deactivated aryl halides and 1-halotetralenes. The method shows good regioselectivity towards ortho substituted halides. Alkali metal carbonates (Li2CO3/Na2CO3/K2CO3/Cs2CO3) were used without a transition metal co-catalyst and ligand. The method is simple, straight-forward and proceeds to afford products in good isolated yields. The method holds potential for future applications in organic synthesis.

Tetrahedron Letters published new progress about Alkyl aryl ethers Role: SPN (Synthetic Preparation), PREP (Preparation). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, COA of Formula: C8H7ClO2.

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

Capkova, Katerina; Yoneda, Yoshiyuki; Dickerson, Tobin J.; Janda, Kim D. published the artcile< Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors>, Formula: C8H7ClO2, the main research area is chlorocinnamic acid hydroxamate preparation BoNT A protease inhibitor activity; hydroxamate chlorocinnamic acid preparation structure activity relationship.

Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure-activity relationship of a series of hydroxamate botulinum neurotoxin A (BoNT/A) protease inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, e.g., I, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.

Bioorganic & Medicinal Chemistry Letters published new progress about Biological warfare agents. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Formula: C8H7ClO2.

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

Hafner, Andreas; Meisenbach, Mark; Sedelmeier, Joerg published the artcile< Flow Chemistry on Multigram Scale: Continuous Synthesis of Boronic Acids within 1 s>, Recommanded Product: 4-Chloro-2-methoxybenzaldehyde, the main research area is multigram scale boronic acid chem synthesis.

The benefits and limitations of a simple continuous flow setup for handling and performing of organolithium chem. on the multigram scale is described. The developed metalation platform embodies a valuable complement to existing methodologies, as it combines the benefits of Flash Chem. (chem. synthesis on a time scale of <1 s) with remarkable throughput (g/min) while mitigating the risk of blockages. Organic Letters published new progress about Boronic acids Role: SPN (Synthetic Preparation), PREP (Preparation). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Recommanded Product: 4-Chloro-2-methoxybenzaldehyde.

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