Category: 53581-86-5

Zhang, Zhi-Jun; Zhou, Xu; Li, Dashan; Chen, Yang; Xiao, Wen-Wen; Li, Rong-Tao; Shao, Li-Dong published the artcile< Aerobic Copper-Catalyzed Intramolecular Cascade Oxidative Isomerization/[4+4] Cyclization of 2,2'-Disubstituted Stilbenes>, Related Products of 53581-86-5, the main research area is dibenzofurofuran benzofuroindole dibenzothienofuran diastereoselective preparation; copper catalyst stereoselective oxidative isomerization cyclization hydroxystilbene; mechanism tandem stereoselective oxidative isomerization cyclization hydroxystilbene.

An aerobic copper-catalyzed cascade oxidative isomerization/[4+4] cyclization of 2,2′-disubstituted stilbenes such as I is described. Under the mild CuCl/N,N’-di-tert-butyl-1,2-ethanediamine (DBED)/air catalytic system, various 5,10-heteroatom-containing tetrahydroindeno[2,1-a]indenes such as dibenzofurofuran II were efficiently prepared through the difunctionalizations of alkenes in a highly atom economic manner. Mechanistic investigations suggested the bicyclic product was likely formed through a sequence of rapid single-electron oxidation/[4+4] cyclization from 2,2′-disubstituted stilbene. The antarafacial manner of the thermally allowed [4+4] cyclization was further proven by series of control experiments and d. functional theory calculations Our findings provide an important addition to the aerobic copper-catalyzed oxidative cyclization.

Journal of Organic Chemistry published new progress about Benzofurans Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation) (benzofuro-). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Related Products of 53581-86-5.

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

Williams, John D.; Khan, Atiyya R.; Cardinale, Steven C.; Butler, Michelle M.; Bowlin, Terry L.; Peet, Norton P. published the artcile< Small molecule inhibitors of anthrax lethal factor toxin>, Category: chlorides-buliding-blocks, the main research area is anthrax lethal factor toxin quinoline structure activity preparation; Anthrax; Bacillus anthracis; Botulinum neurotoxin A; Desymmetrized; Hybrid compound; Lethal factor; Light chain; Matrix metalloprotease; Quinoline; Zinc metalloprotease.

This manuscript describes the preparation of new small mol. inhibitors of Bacillus anthracis lethal factor. The authors’ starting point was the sym., bis-quinolinyl compound (I) (NSC 12155). Optimization of one half of this mol. led to new LF inhibitors that were desymmetrized to afford more drug-like compounds

Bioorganic & Medicinal Chemistry published new progress about Anthrax lethal factors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Category: chlorides-buliding-blocks.

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

Song, Ming-Yu; Cao, Chen-Yu; He, Qiu-Rui; Dong, Qing-Miao; Li, Ding; Tang, Jiang-Jiang; Gao, Jin-Ming published the artcile< Constructing novel dihydrofuran and dihydroisoxazole analogues of isocombretastatin-4 as tubulin polymerization inhibitors through [3+2] reactions>, Application In Synthesis of 53581-86-5, the main research area is dihydrofuran dihydroisoxazole isocombretastatin analog preparation tubulin polymerization inhibitor; Combretastatin-4; Dihydrofuran; Dihydroisoxazole; Isocombretastatin-4; Tubulin polymerization inhibitors; [3+2] reactions.

[3+2] Reactions play a key role in constructing various pharmaceutical moleculars. In this study, using Mn(OAc)3 mediated and 1,3-dipolar [3+2] cyclization reactions, 38 novel dihydrofuran and dihydroisoxazole analogs of isoCA-4 were synthesized as inhibitors of tubulin polymerization Among them, compound 6g (5-(3-(4-chlorophenyl)-5-(3,4,5-trimethoxyphenyl)-4,5-dihydroisoxazol-5-yl)-2-methoxyphenol) was found to be the most potent cytotoxic agents against PC-3 cells with IC50 value of 0.47 μM, and compound 5p ((5-(3-hydroxy-4-methoxyphenyl)-2-phenyl-5-(3,4,5-trimethoxyphenyl)-4,5-dihydrofuran-3-yl)(phenyl)methanone) exhibted highest activity on HeLa cells with IC50 vaule of 2.32 μM. Tubulin polymerization assay revealed that 6g was a dose-dependent and effective inhibitor of tubulin assembly. Immunohistochem. studies and cell cycle distribution anal. indicated that 6g severely disrupted microtubule network and significantly arrested most cells in the G2/M phase of the cell cycle in PC-3 cells. In addition, mol. docking studies showed that two chiral isomers of 6g can bind efficiently and similarly at colchicine binding site of tubulin.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Application In Synthesis of 53581-86-5.

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

Wang, Yi; Fang, Zaixiang; Chen, Xiaochuan; Wang, Yuanhua published the artcile< Dirhodium(II)-Catalyzed C(sp2)-H Azidation of Benzaldehydes>, Safety of 4-Chloro-2-methoxybenzaldehyde, the main research area is dirhodium complex catalyst preparation crystal structure; aldehyde trimethylsilyl azide regioselective dirhodium complex catalyst; azido aldehyde preparation; aromatic aldehydes; azidation; dirhodium; one-electron oxidation; radicals.

An efficient azidation method mediated by dirhodium(II) catalysts to achieve the direct aryl azidation of aromatic aldehydes avoiding the simultaneous use of protected aldehydes and prefunctionalized arenes was reported. The regioselectivity of this method was similar to those of typical aromatic electrophilic substitution reactions. The resulting azidobenzaldehyde products were versatile building blocks or precursors for the synthesis of many biol. active compounds The mechanism studies indicated that the one-electron oxidative intermediate Rh2(II,III)N3 was responsible for the azide transfer.

Chemistry – A European Journal published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 53581-86-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO2, Safety of 4-Chloro-2-methoxybenzaldehyde.

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

Yoshikawa, Kenji; Yokomizo, Aki; Naito, Hiroyuki; Haginoya, Noriyasu; Kobayashi, Shozo; Yoshino, Toshiharu; Nagata, Tsutomu; Mochizuki, Akiyoshi; Osanai, Ken; Watanabe, Kengo; Kanno, Hideyuki; Ohta, Toshiharu published the artcile< Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: Exploration of 5-6 fused rings as alternative S1 moieties>, Recommanded Product: 4-Chloro-2-methoxybenzaldehyde, the main research area is cis diamino cyclohexane derivative factor Xa inhibitor structure.

A series of cis-1,2-diaminocyclohexane derivatives were synthesized with the aim of optimizing previously disclosed factor Xa (fXa) inhibitors. The exploration of 5-6 fused rings as alternative S1 moieties resulted in two compounds which demonstrated improved solubility and reduced food effect compared to the clin. candidate, compound A. Herein, we describe the synthesis and structure-activity relationship (SAR), together with the physicochem. properties and pharmacokinetic (PK) profiles of some prospective compounds

Bioorganic & Medicinal Chemistry published new progress about Anticoagulants. 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

Aldous, F. A. B.; Barrass, B. C.; Brewster, K.; Buxton, D. A.; Green, D. M.; Pinder, R. M.; Rich, P.; Skeels, M.; Tutt, K. J. published the artcile< Structure-activity relations in psychotomimetic phenylalkylamines>, Synthetic Route of 53581-86-5, the main research area is psychotomimetic phenylalkylamine; hypothermia behavior phenylalkylamine.

A series of 48 title compounds were tested for the ability to produce hypothermia in rabbits as a qual. screen for psychotomimetic activity. Addnl. tests of the ability to mimic LSD [50-37-3], mescaline [54-04-6], and DOM (2,5-dimethoxy-4-methylamphetamine [15588-95-1] in the cat EEG, as well as behavioral responses in rats, permitted a reliable quant. anal. to be made of structure-activity relations in these drugs. Trans-2-(2,5-dimethoxy-4-methylphenyl)cyclopropylamine-HCl (I-HCl) [53581-71-8] produced the full LSD-like response and was about a third as potent as DOM.

Journal of Medicinal Chemistry published new progress about Behavior. 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

Xiao, Peihong; Tang, Zhixing; Wang, Kai; Chen, Hua; Guo, Qianyou; Chu, Yang; Gao, Lu; Song, Zhenlei published the artcile< Chemoselective Reduction of Sterically Demanding N,N-Diisopropylamides to Aldehydes>, COA of Formula: C8H7ClO2, the main research area is aldehyde preparation sterically demanding diisopropylamide chemoselective reduction.

A sequential one-pot process for chemoselectively reducing sterically demanding N,N-diisopropylamides to aldehydes has been developed. In this reaction, amides are activated with EtOTf to form imidates, which are reduced with LiAlH(OR)3 [R = t-Bu, Et] to give aldehydes by hydrolysis of the resulting hemiaminals. The non-nucleophilic base 2,6-DTBMP remarkably improves reaction efficiency. The combination of EtOTf/2,6-DTBMP and LiAlH(O-t-Bu)3 was found to be optimal for reducing alkyl, alkenyl, alkynyl, and 2-monosubstituted aryl N,N-diisopropylamides. In contrast, EtOTf and LiAlH(OEt)3 in the absence of base were found to be optimal for reducing extremely sterically demanding 2,6-disubstituted N,N-diisopropylbenzamides. The reaction tolerates various reducible functional groups, including aldehyde and ketone. 1H NMR studies confirmed the formation of imidates stable in water. The synthetic usefulness of this methodol. was demonstrated with N,N-diisopropylamide-directed ortho-metalation and C-H bond activation.

Journal of Organic Chemistry published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), 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