Category: 531-88-4

Lei, Zhen-Yao; Hu, Kui; He, Yuan-Xiang; Geng, Shu; Chen, Li-Na; Zou, Shuai; Pan, Li; Ding, Zhi-Jun; Huang, Feng published the artcile< Visible light-induced N-radical 5-exo/6-endo cyclization of alkenyl amides: facile access to isoindolinones/isoquinolinones>, Formula: C10H10O4, the main research area is isoindolinone isoquinolinone preparation; alkenyl amide visible light radical cyclization.

An efficient N-centered radical intramol. cyclization reaction of alkenyl amides induced by visible light was described. In this process, an alkenyl amide underwent 5-exo/6-endo cyclization to selectively yield two critical alkaloid structures, namely isoindolinones and isoquinolinones.

Organic & Biomolecular Chemistry published new progress about Amides Role: RCT (Reactant), RACT (Reactant or Reagent) (alkenyl). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Formula: C10H10O4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Li, Junxuan; Zhou, Jinlei; Wang, Yumei; Yu, Yue; Liu, Qiang; Yang, Tilong; Chen, Huoji; Cao, Hua published the artcile< Mechanistic insight into the synergistic Cu/Pd-catalyzed carbonylation of aryl iodides using alcohols and dioxygen as the carbonyl source>, SDS of cas: 531-88-4, the main research area is aryl iodide alc carbonylation dioxygen carbonyl source mechanistic insight.

Pd-catalyzed carbonylation, as an efficient synthetic approach for the installation of carbonyl groups in organic compounds, has been one of the most important research fields in the past decade. Although elegant reactions that allow highly selective carbonylations have been developed, straightforward routes with improved reaction activity and broader substrate scope remain long-term challenges for new practical applications. Here, authors show a new type of synergistic Cu/Pd-catalyzed carbonylation reaction using alcs. and dioxgen as the carbonyl sources. A broad range of aryl iodides and alcs. are compatible with this protocol. The reaction is concise and practical due to the ready availability of the starting materials and the scalability of the reaction. In addition, the reaction affords lactones and lactams in an intermol. fashion. Moreover, DFT calculations have been performed to study the detailed mechanisms.

Science China: Chemistry published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, SDS of cas: 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Liu, Zhuoling; Cong, Shiqing; Tan, Zhenghuai; Deng, Yong published the artcile< Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease>, Computed Properties of 531-88-4, the main research area is benzylidene benzyl phthalide Mannich base preparation Alzheimers disease treatment; 3-benzylidene/benzylphthalide Mannich base derivatives; AChE inhibitors; Alzheimer’s disease; Antioxidants; MAO-B inhibitors; Multifunctional anti-AD agents.

To discover novel multifunctional agents for the treatment of Alzheimer’s disease, a series of 3-benzylidene/benzylphthalide Mannich base derivatives were designed, synthesized and evaluated. The biol. screening results indicated that most of these derivatives exhibited good multifunctional activities. Among them, compound (Z)-13c (I) raised particular interest because of its excellent multifunctional bioactivities. It displayed excellent EeAChE and HuAChE inhibition (IC50 = 9.18 x 10-5 and 6.16 x 10-4 μM, resp.), good MAO-B inhibitory activity (IC50 = 5.88μM) and high antioxidant activity (ORAC = 2.05 Trolox equivalent). Addnl., it also exhibited good antiplatelet aggregation activity, moderate self- and Cu2+-induced Aβ1-42 aggregation inhibitory potency, disaggregation ability on Aβ1-42 fibrils, biometal chelating ability, appropriate BBB permeability and significant neuroprotective effect. Furthermore, (Z)-13c can also ameliorate the learning and memory impairment induced by scopolamine in mice. These multifunctional properties highlight compound (Z)-13c as a promising candidate for further development of multifunctional drug against AD.

Bioorganic & Medicinal Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Computed Properties of 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Takakura, Ryoya; Ban, Kazuho; Sajiki, Hironao; Sawama, Yoshinari published the artcile< Platinum-on-Carbon-Catalyzed Aqueous Oxidative Lactonization of Diols by Using Molecular Oxygen>, Category: benzofurans, the main research area is lactone preparation green chem; diol oxidative lactonization platinum catalyst.

A lactonization of various diols e.g., I catalyzed by platinum on carbon (Pt/C) in water under an atm. of mol. oxygen was developed. Diols e.g., I were transformed into lactones e.g., II by the present oxidative lactonization method.

Synlett published new progress about Glycols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Category: benzofurans.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ye, Chanyuan; Xu, Rui; Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Shi, Yichun; Liu, Zhuoling; Liu, Xiuxiu; Deng, Yong published the artcile< Design, synthesis, and in vitro evaluation of 4-aminoalkyl-1(2H)-phthalazinones as potential multifunctional anti-Alzheimer's disease agents>, Application of C10H10O4, the main research area is aminoalkylphthalazinone preparation cholinesterase inhibitor SAR antioxidant neuroprotective Alzheimer disease; 4-(aminoalkyl)-1(2H)-phthalazinone derivatives; Acetylcholinesterase inhibitors; Alzheimer’s disease; Anti-neuroinflammation; Aβ aggregation inhibitors; Monoamine oxidases inhibitors; Multifunctional agents.

A series of 4-aminoalkyl-1(2H)-phthalazinone derivatives I (R1 = benzyl, 2-methoxybenzyl, 2-dimethylaminobenzyl, 4-dimethylaminobenzyl, ethyl; R2 = Me, Et; R1R2 = -(CH2)5-, -(CH2)2O(CH2)2-, -(CH2)2N(CH3)(CH2)2-; n = 1, 3, 5) was designed and synthesized as potential multifunctional agents for Alzheimer’s disease (AD) treatment. In vitro biol. assay results demonstrated that most synthesized compounds I exhibited significant AChE inhibition, moderate to high monoamine oxidases (MAO) inhibitory potencies and good anti-platelet aggregation abilities. Among them, compound I (R1 = Bn; R2 = Et; n = 3) (II) exhibited the highest inhibitory potencies towards MAO-B and MAO-A (IC50 = 0.7μM and 6.4μM resp.), moderate inhibition towards AChE (IC50 = 8.2μM), and good activities against self- and Cu2+-induced Aβ1-42 aggregation and platelet aggregation. Moreover, II also displayed antioxidant capacity, neuroprotective potency, anti-neuroinfammation and BBB permeability. These excellent results indicated that compound II could be worthy of further studies to be considered as a promising multifunctional candidate for the treatment of AD.

Bioorganic Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Application of C10H10O4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cai, Lingchao; Zhang, Kui; Chen, Shuming; Lepage, Romain J.; Houk, K. N.; Krenske, Elizabeth H.; Kwon, Ohyun published the artcile< Catalytic Asymmetric Staudinger-aza-Wittig Reaction for the Synthesis of Heterocyclic Amines>, Category: benzofurans, the main research area is amine heterocycle preparation catalyst asym Staudinger aza Wittig.

Many natural products and medicinal drugs are heterocyclic amines possessing a chiral quaternary carbon atom in their heterocyclic ring. Herein, the authors report the first catalytic and asym. Staudinger-aza-Wittig reaction for the desymmetrization of ketones. This highly enantioselective transformation proceeds at room temperature to provide high yields-even on multigram scales-of nitrogen heterocycles featuring a chiral quaternary center. The products of this reaction are potential precursors for the synthesis of pharmaceuticals. A com. available small P-chiral phosphine catalyst, HypPhos, induces the asymmetry and is recycled through in situ reduction of its oxide, mediated by phenylsilane in the presence of a carboxylic acid. The efficiency, selectivity, scalability, mild reaction conditions, and broad substrate scope portend that this process will expedite the syntheses of chiral heterocyclic amines of significance to chem., biol., and medicine.

Journal of the American Chemical Society published new progress about Aromatic heterocyclic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Category: benzofurans.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ibrahimi, Maroua; Khoumeri, Omar; Abderrahim, Raoudha; Terme, Thierry; Vanelle, Patrice published the artcile< Synthesis of 3-Benzylphthalide Derivatives by Using a TDAE Strategy>, HPLC of Formula: 531-88-4, the main research area is benzylphthalide preparation; nitrobenzyl chloride tetrakisdimethylaminoethylene formylbenzoate nucleophilic addition.

A one-pot synthesis of new 3-benzylphthalide derivatives I (X = CH, N; R1 = 4-NO2, 3-OMe-4-NO2, 2-NO2-4-C6H4, etc.; R2 = 4-CN, 5-Cl, 4-COOMe, etc.) was developed by using a strategy based on tetrakis(dimethylamino)ethylene (TDAE). The reactions in the presence of TDAE of substituted benzyl chlorides with Me 2-formylbenzoate or of substituted methyl-2-formylbenzoates with 4-nitrobenzyl chloride furnished the corresponding isobenzofuran-1(3H)-one products in moderate to good yields.

Synlett published new progress about Benzaldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, HPLC of Formula: 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ye, Chanyuan; Xu, Rui; Cao, Zhongcheng; Song, Qing; Yu, Guangjun; Shi, Yichun; Liu, Zhuoling; Liu, Xiuxiu; Deng, Yong published the artcile< Design, synthesis, and in vitro evaluation of 4-aminoalkyl-1(2H)-phthalazinones as potential multifunctional anti-Alzheimer's disease agents>, Application of C10H10O4, the main research area is aminoalkylphthalazinone preparation cholinesterase inhibitor SAR antioxidant neuroprotective Alzheimer disease; 4-(aminoalkyl)-1(2H)-phthalazinone derivatives; Acetylcholinesterase inhibitors; Alzheimer’s disease; Anti-neuroinflammation; Aβ aggregation inhibitors; Monoamine oxidases inhibitors; Multifunctional agents.

A series of 4-aminoalkyl-1(2H)-phthalazinone derivatives I (R1 = benzyl, 2-methoxybenzyl, 2-dimethylaminobenzyl, 4-dimethylaminobenzyl, ethyl; R2 = Me, Et; R1R2 = -(CH2)5-, -(CH2)2O(CH2)2-, -(CH2)2N(CH3)(CH2)2-; n = 1, 3, 5) was designed and synthesized as potential multifunctional agents for Alzheimer’s disease (AD) treatment. In vitro biol. assay results demonstrated that most synthesized compounds I exhibited significant AChE inhibition, moderate to high monoamine oxidases (MAO) inhibitory potencies and good anti-platelet aggregation abilities. Among them, compound I (R1 = Bn; R2 = Et; n = 3) (II) exhibited the highest inhibitory potencies towards MAO-B and MAO-A (IC50 = 0.7μM and 6.4μM resp.), moderate inhibition towards AChE (IC50 = 8.2μM), and good activities against self- and Cu2+-induced Aβ1-42 aggregation and platelet aggregation. Moreover, II also displayed antioxidant capacity, neuroprotective potency, anti-neuroinfammation and BBB permeability. These excellent results indicated that compound II could be worthy of further studies to be considered as a promising multifunctional candidate for the treatment of AD.

Bioorganic Chemistry published new progress about Alzheimer disease. 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Application of C10H10O4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cai, Lingchao; Zhang, Kui; Chen, Shuming; Lepage, Romain J.; Houk, K. N.; Krenske, Elizabeth H.; Kwon, Ohyun published the artcile< Catalytic Asymmetric Staudinger-aza-Wittig Reaction for the Synthesis of Heterocyclic Amines>, Category: benzofurans, the main research area is amine heterocycle preparation catalyst asym Staudinger aza Wittig.

Many natural products and medicinal drugs are heterocyclic amines possessing a chiral quaternary carbon atom in their heterocyclic ring. Herein, the authors report the first catalytic and asym. Staudinger-aza-Wittig reaction for the desymmetrization of ketones. This highly enantioselective transformation proceeds at room temperature to provide high yields-even on multigram scales-of nitrogen heterocycles featuring a chiral quaternary center. The products of this reaction are potential precursors for the synthesis of pharmaceuticals. A com. available small P-chiral phosphine catalyst, HypPhos, induces the asymmetry and is recycled through in situ reduction of its oxide, mediated by phenylsilane in the presence of a carboxylic acid. The efficiency, selectivity, scalability, mild reaction conditions, and broad substrate scope portend that this process will expedite the syntheses of chiral heterocyclic amines of significance to chem., biol., and medicine.

Journal of the American Chemical Society published new progress about Aromatic heterocyclic amines Role: SPN (Synthetic Preparation), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, Category: benzofurans.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ibrahimi, Maroua; Khoumeri, Omar; Abderrahim, Raoudha; Terme, Thierry; Vanelle, Patrice published the artcile< Synthesis of 3-Benzylphthalide Derivatives by Using a TDAE Strategy>, HPLC of Formula: 531-88-4, the main research area is benzylphthalide preparation; nitrobenzyl chloride tetrakisdimethylaminoethylene formylbenzoate nucleophilic addition.

A one-pot synthesis of new 3-benzylphthalide derivatives I (X = CH, N; R1 = 4-NO2, 3-OMe-4-NO2, 2-NO2-4-C6H4, etc.; R2 = 4-CN, 5-Cl, 4-COOMe, etc.) was developed by using a strategy based on tetrakis(dimethylamino)ethylene (TDAE). The reactions in the presence of TDAE of substituted benzyl chlorides with Me 2-formylbenzoate or of substituted methyl-2-formylbenzoates with 4-nitrobenzyl chloride furnished the corresponding isobenzofuran-1(3H)-one products in moderate to good yields.

Synlett published new progress about Benzaldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 531-88-4 belongs to class benzofurans, and the molecular formula is C10H10O4, HPLC of Formula: 531-88-4.

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem