Day: October 13, 2022

Henderson, Scott H.; West, Ryan A.; Ward, Simon E.; Honey, Mark A. published the artcile< Metal-free selective mono-halodecarboxylation of heteroarenes under mild conditions>, Application In Synthesis of 23077-43-2, the main research area is haloheteroarene preparation; heteroarene carboxylic acid mono halodecarboxylation; halodecarboxylation; mild conditions; selective halogenation.

A mild and efficient protocol was developed for the synthesis of haloheteroarenes such as I [R = H, 5-F, 5-NO2, etc.; R1 = Cl, Br; X = C, N] via mono-halodecarboxylation of heteroarene carboxylic acids by treatment with N-bromosuccinimide or N-chlorosuccinimide. This method was metal-free and displayed significant advantages over traditional halodecarboxylation procedures that require expensive and toxic metal catalysts, basic conditions, time-consuming intermediate isolation and elevated reaction temperatures

Royal Society Open Science published new progress about Decarboxylation (halo). 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Application In Synthesis of 23077-43-2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Palani, Vignesh; Perea, Melecio A.; Gardner, Kristen E.; Sarpong, Richmond published the artcile< A pyrone remodeling strategy to access diverse heterocycles: application to the synthesis of fascaplysin natural products>, Safety of Methyl 1H-indole-7-carboxylate, the main research area is fascaplysin preparation; pyridoindole preparation.

The synthesis of diverse N-fused heterocycles, including the pyrido[1,2-a]indole scaffold, e.g., I, using an efficient pyrone remodeling strategy was described. The pyrido[1,2-a]indole core was demonstrated to be a versatile scaffold that could be site-selectively functionalized. The utility of this novel annulation strategy was showcased in a concise formal synthesis of three fascaplysin congeners.

Chemical Science published new progress about Fused heterocyclic compounds Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Safety of Methyl 1H-indole-7-carboxylate.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Iioka, Ryoya; Yorozu, Kohei; Sakai, Yoko; Kawai, Rika; Hatae, Noriyuki; Takashima, Katsuki; Tanabe, Genzoh; Wasada, Hiroaki; Yoshimatsu, Mitsuhiro published the artcile< Synthesis of azepino[1,2-a]indole-10-amines via [6+1] annulation of ynenitriles with Reformatsky reagent>, Category: indole-building-block, the main research area is azepinoindoleamine preparation annulation Lewis acid catalysis.

Lewis acid-catalyzed [6+1] annulation reactions of 2-cyano-1-propargyl- and 2-alkynyl-1-cyanomethyl-indoles with Reformatsky reagent are described. 8-Aryl, 8-alkyl-, 8-hetaryl-, 9-aryl, and 9-alkyl-azepino[1,2-a]indole amines were obtained through a 7-endo-mode cyclization of the β-aminoacrylate intermediates. The antiproliferative activity of the azepino[1,2-a]indoles analogs against the HCT-116 cells were also examined

European Journal of Organic Chemistry published new progress about Antitumor agents. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Category: indole-building-block.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Tran, Quy Thi Ngoc; Lee, Regina Ching Hua; Liu, Hon Jin; Ran, Danli; Low, Vincent Zhan Lin; To, Dong Quang; Chu, Justin Jang Hann; Chai, Christina Li Lin published the artcile< Discovery and development of labdane-oxindole hybrids as small-molecule inhibitors against chikungunya virus infection>, COA of Formula: C8H6ClNO, the main research area is chikungunya virus infection labdane oxindole hybrid; Antiviral; Arbovirus; Chikungunya; Labdane diterpenoid; Oxindole.

Chikungunya virus (CHIKV) infection, a febrile illness caused by a mosquito-transmitted alphavirus, has afflicted millions of people worldwide. There is currently no approved effective antiviral treatment for CHIKV infection. In this study, we report a new class of small-mol. CHIKV inhibitors, the oxindole-labdanes, that potently block the replication of CHIKV with good selectivity. Andrographolide, a previously reported inhibitor of CHIKV infection, was used as the lead compound for our initial structure-activity relationship (SAR) study. From a focused library of 72 andrographolide analogs, we identified the lead compound (E)-2 with improved antiviral activities. Further optimization of (E)-2 led to the discovery of the normal-labdane 7-chloro-oxindole (E)-42 as potent inhibitor against two low-passage CHIKV isolates from human patients with an EC50 of 1.55 μM against CHIKV-122508 and 0.14 μM against CHIKV-6708. Compound (E)-42 displayed minimal cytotoxic liability (CC50 > 100 μM), thus furnishing good selectivity relative to the host cells. Mechanistically, (E)-42 does not inactivate the viral particles but rather acts on the host cells to interfere with the viral replication, demonstrating both prophylactic and therapeutic effects. Our findings open a new avenue for the development of oxindole-labdane compounds as promising antiviral drugs against CHIKV infection.

European Journal of Medicinal Chemistry published new progress about Antiviral agents. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, COA of Formula: C8H6ClNO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Yoo, Woo-Jin; Capdevila, Montse Guiteras; Du, Xiangwei; Kobayashi, Shu published the artcile< Base-Mediated Carboxylation of Unprotected Indole Derivatives with Carbon Dioxide>, Computed Properties of 23077-43-2, the main research area is indole carboxylic acid preparation; base carboxylation unprotected indole carbon dioxide.

A simple and straightforward method for the preparation of indole-3-carboxylic acids was discovered through the direct carboxylation of indoles with atm. pressure of carbon dioxide (CO2) under basic conditions. The key for the reaction was found to be the use of a large excess of LiOtBu as a base to suppress the undesired decarboxylation side reaction.

Organic Letters published new progress about Carboxylation. 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Computed Properties of 23077-43-2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Hrizi, Asma; Cailler, Manon; Romdhani-Younes, Moufida; Carcenac, Yvan; Thibonnet, Jerome published the artcile< Synthesis of New Highly Functionalized 1H-Indole-2-carbonitriles via Cross-Coupling Reactions>, Reference of 399-76-8, the main research area is alkenyl indole carbonitrile preparation; aryl indole carbonirile preparation; 1H-indole-2-carbonitriles; Heck; Sonogashira; Stille; Suzuki–Miyaura.

An approach for the preparation of polysubstituted indole-2-carbonitriles through a cross-coupling reaction of compounds 1-(but-2-ynyl)-1H-indole-2-carbonitriles and 1-benzyl-3-iodo-1H-indole-2-carbonitriles was described. The reactivity of indole derivatives with iodine at position 3 was studied using cross-coupling reactions. The Sonogashira, Suzuki-Miyaura, Stille and Heck cross-couplings afforded a variety of di-, tri- and tetra-substituted indole-2-carbonitriles.

Molecules published new progress about Alkenes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Reference of 399-76-8.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wu, Ke-Xin; Xu, Yi-Ze; Cheng, Liang; Wu, Run-Shi; Liu, Peng-Ze; Xu, Da-Zhen published the artcile< Iron-catalyzed oxidative bis-arylation of indolin-2-ones for direct construction of quaternary carbons>, Computed Properties of 20870-77-3, the main research area is oxindole bis indolyl preparation chemoselective green chem; indolinone indole oxidative bis arylation iron catalyst.

A direct construction of all-carbon quaternary centers from secondary C(sp3)-H substrates through a dehydrogenative cross-coupling reaction was described. Using FeCl2·4H2O as the catalyst and employing air (mol. oxygen) as the terminal oxidant, the cross-coupling of indolin-2-ones I (R1 = H, Me, Ph, Bn; R2 = H, 6-Cl, 5-F, etc.) with indoles such as 5-fluoroindole, N-methylindole, 3-methylindole, etc. proceeded smoothly under mild, ligand-free and base-free conditions, providing 3,3-disubstituted oxindoles bearing all-carbon quaternary centers II (R3 = 5-fluoroindol-3-yl, N-methylindol-3-yl, 3-methylindol-2-yl, etc.) with excellent chemoselectivities.

Green Chemistry published new progress about Arylation (chemoselective). 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Computed Properties of 20870-77-3.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Ghosh, Ayndrila; Mandal, Saurodeep; Das, Sujoy; Shaw, Pallab; Chattopadhyay, Ansuman; Sahoo, Prithidipa published the artcile< Insights into the phenomenon of acquisition and accumulation of Fe3+ in Hygrophila spinosa through fluorimetry and fluorescence images>, Product Details of C30H36N4O2, the main research area is Hygrophila ferric uptake fluorescent probe imaging.

Rhodamine functionalized fluorescent probe IP has been synthesized to investigate the phenomenon of Fe3+ acquisition and accumulation in Hygrophila spinosa. H. spinosa is a tropical medicinal plant which is iron rich and consumed for the treatment of the patients suffering from anemia. IP is capable of selectively binding Fe3+ by enhancing fluorescent intensity via “”turn on”” mechanism due to complex formation. Spectroscopic studies and microscopic tools helped in better understanding about the acquisition as well as the quant. accumulation of Fe3+ in different parts of the plant.

Tetrahedron Letters published new progress about Fluorescence imaging. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Product Details of C30H36N4O2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Li, Ruo-Pu; Wang, Zheng-Lin; Zhang, Yun-Hao; Tan, Zhi-Yu; Xu, Da-Zhen published the artcile< Iodine-Catalyzed Oxidative Coupling of Indolin-2-ones with Indoles: Synthesis of 3,3-Disubstituted Oxindole Compounds>, Application of C8H6ClNO, the main research area is disubstituted oxindole preparation; indolinone indole oxidative coupling iodine catalyst.

Here, an iodine-catalyzed oxidative coupling of indolinones with indoles for the construction of compounds with all-carbon quaternary centers such as 1H,1”H-[3,3′:3′,3”-terindol]-2′(1’H)-ones I [R1 = H, Me, Bn, etc.; R2 = H, 5-Br, 5-F, etc.; R3 = H, Me, R4 = H, 2-Me, 5-OMe, etc.] was described. The method performed under metal-free and peroxide-free conditions, providing 3,3-disubstituted oxindoles via two C-C bond formations from secondary C(sp3)-Hs in a straightforward manner.

ChemistrySelect published new progress about C-C bond formation. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Application of C8H6ClNO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Tang, Tengxuan; Wang, Jing; Xu, Dongmei published the artcile< Synthesis of a novel hyperbranched polymer and its application in multi-channel sensing Fe3+>, COA of Formula: C30H36N4O2, the main research area is hyperbranched polymer fluorescent sensor iron.

A novel hyperbranched polymer was designed and synthesized as a spectral probe for Fe3+. The polymer showed high selectivity and sensitivity to Fe3+ in CH3CN/H2O (75/25, volume/volume). Fe3+ caused a new peak at 560 nm in UV-Vis absorption, a 31 nm fluorescence red shift, a 35-fold enhancement in fluorescence intensity at 575 nm and an 8.3-fold enhancement in fluorescence quantum yield, accompanied by a visual color change from colorless to pink and a fluorescence from dark to bright orange. The colorimetric and fluorescent detection limits were 1.29 and 1.88 μM, resp. The detection was almost not interfered by other common metal cations. The polymer could be applied in assaying Fe3+ in real sample with similar precision to that of at. absorption spectroscopy.

Research on Chemical Intermediates published new progress about Colorimetric sensors. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, COA of Formula: C30H36N4O2.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles