Day: February 7, 2023

Palladium-Catalyzed Glycosylation: Novel Synthetic Approach to Diverse N-Heterocyclic Glycosides was written by Ji, Li;Xiang, Shao-Hua;Leng, Wei-Lin;Le Mai Hoang, Kim;Liu, Xue-Wei. And the article was included in Organic Letters in 2015.Recommanded Product: 5-Isopropylindoline-2,3-dione This article mentions the following:

An efficient and highly stereoselective method for the construction of N-heterocyclic glycosides is reported. This method is based on a palladium-catalyzed allylation which proceeded to provide N-heterocyclic glycosyl compounds in good-to-excellent yields with β- or α-selectivity. Various N-nucleophiles were examined for this reaction and selected N-glycosyl isatin substrates were further elaborated to bis-indole sugars which have potential as antiproliferative drugs. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Recommanded Product: 5-Isopropylindoline-2,3-dione).

5-Isopropylindoline-2,3-dione (cas: 150560-58-0) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Recommanded Product: 5-Isopropylindoline-2,3-dione

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

Optimization, Structure-Activity Relationship, and Mode of Action of Nortopsentin Analogues Containing Thiazole and Oxazole Moieties was written by Guo, Jincheng;Hao, Yanan;Ji, Xiaofei;Wang, Ziwen;Liu, Yuxiu;Ma, Dejun;Li, Yongqiang;Pang, Huailin;Ni, Jueping;Wang, Qingmin. And the article was included in Journal of Agricultural and Food Chemistry in 2019.Computed Properties of C9H5BrN2 This article mentions the following:

Plant diseases seriously endanger plant health, and it is very difficult to control them. A series of nortopsentin analogs were designed, synthesized, and evaluated for their antiviral activities and fungicidal activities. Most of these compounds displayed higher antiviral activities than ribavirin. Compounds (CAS 224434-76-8, 265110-91-6, 272104-33-3), with excellent antiviral activities, emerged as novel antiviral lead compounds, among which compound (CAS 265110-91-6) was selected for further antiviral mechanism research. The mechanism research results indicated that these compounds may play an antiviral role by aggregating viral particles to prevent their movement in plants. Further fungicidal activity tests revealed that nortopsentin analogs displayed broad-spectrum fungicidal activities. Compounds (CAS 2376842-39-4 and 2376840-03-6) displayed higher antifungal activities against Alternaria solani than the com. fungicides carbendazim and chlorothalonil. Current research has laid a foundation for the application of nortopsentin analogs in plant protection. In the experiment, the researchers used many compounds, for example, 5-Bromo-3-cyanoindole (cas: 90271-86-6Computed Properties of C9H5BrN2).

5-Bromo-3-cyanoindole (cas: 90271-86-6) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Computed Properties of C9H5BrN2

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

In situ preparation of a ferric polymeric aluminum chloride-silica gel nanocatalyst by mechanical grinding and its solid-phase catalytic behavior in organic synthesis was written by Liang, Yuwang;Wang, Gang;Li, Xiang;Zhang, Qiuping;Zhan, Haijuan;Bi, Shuxian;Wu, Zhiqiang;Liu, Wanyi. And the article was included in New Journal of Chemistry in 2022.Synthetic Route of C8H6N2O2 This article mentions the following:

In recent years, clean and sustainable mechanochem. solvent-free reactions have emerged as a viable alternative to solution chem. In order to completely solve the problem of environmental pollution caused by solvents and surfactants in LASC and LASSC systems, a green method for the in situ preparation of environmentally friendly inorganic polymeric Lewis acids and silica gel as nanocatalysts (PLASC) under solvent-free mech. grinding conditions was designed and realized by mechanochem. means, which is simple to operate and the process generates no other waste. Subsequently, 3-alkylindole derivatives (35-75%), β-amino alc. derivatives (90%), benzimidazole derivatives (85-90%) and quinoxaline derivatives (93-99%) were synthesized by a one-pot cooking method under continuous grinding conditions. The mechanism of in situ self-assembly of PAFC and silica gel on the silica gel surface under mech. forces and the new catalytically active species-Si-O-Al(Fe) polynuclear metal complexes resulting from chem. reforming were discovered and confirmed by SEM, HR-TEM, FT-IR, XRD and XPS tests as well as by solution morphol. studies. The true active center -O-Fe-O-Si-O-/-O-Si-O-Al-O- chem. bonding unit was revealed and found to be a nanoscale fibrous structure that is highly stable and can be reused at least 10 times without deactivation. The PLASC catalyst has remarkable green chem. properties such as easy recycling and a very low E factor, making it a new type of cheap, efficient and green catalyst. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Synthetic Route of C8H6N2O2).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Synthetic Route of C8H6N2O2

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

Synthesis and antioxidant activity evaluations of melatonin-based analogue indole-hydrazide/hydrazone derivatives was written by Yilmaz, Ayse Didem;Coban, Tulay;Suzen, Sibel. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2012.Product Details of 827-01-0 This article mentions the following:

Melatonin (MLT) is a hormone synthesized from the pineal gland. It is a direct scavenger of free radicals, which is related to its ability to defend cells from oxidative stress. Recently MLT-related compounds are under investigation to establish which ones exhibit the maximum activity with the lowest side effects. In this study, 5-chloroindole hydrazide/hydrazone derivatives were synthesized from 5-chloroindole-3-carboxaldehyde and phenylhydrazine derivatives All the compounds were characterized and in vitro antioxidant activity was investigated against MLT and BHT. Most of the compounds showed strong inhibitory effect on the superoxide radical scavenging assay at 1 mM concentration (79 to 95%). Almost all the tested compounds possessed strong scavenging activity against the DPPH radical scavenging activity with IC₅₀ values (2 to 60 μM). Lastly, compound (E)-I revealed stronger inhibitory activity against MLT in the LP inhibitory assay at 0.1mM concentration (51%) while the rest of the compounds showed moderate inhibition. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Product Details of 827-01-0).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Product Details of 827-01-0

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

Palladium-mediated in situ synthesis of an anticancer agent was written by Indrigo, Eugenio;Clavadetscher, Jessica;Chankeshwara, Sunay V.;Lilienkampf, Annamaria;Bradley, Mark. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2016.Product Details of 754214-56-7 This article mentions the following:

As a novel prodrug activation strategy Pd(0) nanoparticles, entrapped within a modular polymeric support, were used in cell culture, to synthesize the anticancer agent PP-121 from two non-toxic precursors, thereby inducing cell death in the first example of in situ mediated drug synthesis. In the experiment, the researchers used many compounds, for example, 7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7Product Details of 754214-56-7).

7-Azaindole-5-boronic Acid Pinacol Ester (cas: 754214-56-7) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Product Details of 754214-56-7

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

A study of the mechanism of the azidophenylselenylation of glycals was written by Mironov, Yu. V.;Grachev, A. A.;Lalov, A. V.;Sherman, A. A.;Egorov, M. P.;Nifantiev, N. E.. And the article was included in Russian Chemical Bulletin in 2010.Computed Properties of C14H9NO2S This article mentions the following:

Chem. and physicochem. studies of homogeneous azidophenylselenylation of glycols with diacetoxyiodobenzene, trimethylsilyl azide, and di-Ph diselenide in dichloromethane revealed that the most probable key reaction step is the formation of phenylselenyl azide, an azide radical donor. A method for azidophenylsulfenylation of glycals, e.g. I, with diacetoxyiodobenzene, di-Ph diselenide, and sodium azide to give the corresponding glycosides, e.g. II, was proposed. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Computed Properties of C14H9NO2S).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Computed Properties of C14H9NO2S

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

Copper-Mediated Decarboxylative Coupling between Arylacetic Acids and 1,3-Dicarbonyl Compounds was written by Wu, Yinrong;Wen, Kangmei;Chen, Jiewen;Shi, Jie;Yao, Xingang;Tang, Xiaodong. And the article was included in Organic Letters in 2021.Computed Properties of C10H8ClNO2 This article mentions the following:

A copper-mediated decarboxylative coupling reaction between arylacetic acids and 1,3-dicarbonyl compounds was described for the synthesis of ((indolyl)methyl)-oxocycloalkyl-esters, e.g., I. Significantly, methanocycloocta[b]indoles II [R = COOEt, CONHEt, SO₂Ph, etc.; R¹ = H, 4-Cl, 5-Br, etc.] were also obtained by sequential intramol. dehydrocyclization process in some cases. This protocol featured a broad substrate scope, simple operations, and good yields. Moreover, the products exhibited potent antiproliferative activity against the human cancer cell lines by a MTT assay. In the experiment, the researchers used many compounds, for example, 2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4Computed Properties of C10H8ClNO2).

2-(5-Chloro-1H-indol-3-yl)acetic acid (cas: 1912-45-4) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Computed Properties of C10H8ClNO2

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

The use of anhydrous CeCl₃ as a catalyst for the synthesis of 3-sulfenyl indoles was written by Silveira, Claudio C.;Mendes, Samuel R.;Wolf, Lucas;Martins, Guilherme M.. And the article was included in Tetrahedron Letters in 2010.Formula: C14H9NO2S This article mentions the following:

Anhydrous CeCl₃ was successfully used as a catalyst for the synthesis of several 3-sulfenyl indoles in good to excellent yields through the reaction of indoles with N-(alkylthio) and N-(arylthio)phthalimides in DMF. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Formula: C14H9NO2S).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Formula: C14H9NO2S

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

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains was written by Hay, Duncan A.;Fedorov, Oleg;Martin, Sarah;Singleton, Dean C.;Tallant, Cynthia;Wells, Christopher;Picaud, Sarah;Philpott, Martin;Monteiro, Octovia P.;Rogers, Catherine M.;Conway, Stuart J.;Rooney, Timothy P. C.;Tumber, Anthony;Yapp, Clarence;Filippakopoulos, Panagis;Bunnage, Mark E.;Muller, Susanne;Knapp, Stefan;Schofield, Christopher J.;Brennan, Paul E.. And the article was included in Journal of the American Chemical Society in 2014.Related Products of 4583-55-5 This article mentions the following:

Small-mol. inhibitors that target bromodomains outside of the bromodomain and extra-terminal (BET) sub-family are lacking. Here, the authors describe highly potent and selective ligands for the bromodomain module of the human lysine acetyl transferase CBP/p300, developed from a series of 5-isoxazolyl-benzimidazoles. The starting point was a fragment hit, which was optimized into a more potent and selective lead using parallel synthesis employing Suzuki couplings, benzimidazole-forming reactions, and reductive aminations. The selectivity of the lead compound against other bromodomain family members was investigated using a thermal stability assay, which revealed some inhibition of the structurally related BET family members. To address the BET selectivity issue, x-ray crystal structures of the lead compound bound to the CREB binding protein (CBP) and the first bromodomain of BRD4 (BRD4(1)) were used to guide the design of more selective compounds The crystal structures obtained revealed two distinct binding modes. By varying the aryl substitution pattern and developing conformationally constrained analogs, selectivity for CBP over BRD4(1) was increased. The optimized compound is highly potent (K_d = 21 nM) and selective, displaying 40-fold selectivity over BRD4(1). Cellular activity was demonstrated using fluorescence recovery after photo-bleaching (FRAP) and a p53 reporter assay. The optimized compounds are cell-active and have nanomolar affinity for CBP/p300; therefore, they should be useful in studies investigating the biol. roles of CBP and p300 and to validate the CBP and p300 bromodomains as therapeutic targets. In the experiment, the researchers used many compounds, for example, 5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5Related Products of 4583-55-5).

5-Bromo-2,3-dimethyl-1H-indole (cas: 4583-55-5) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Related Products of 4583-55-5

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

Carbene and radical pathways in pyrolysis of benzisoxazolones and benzotriazoles was written by Prager, Rolf H.;Baradarani, Mehdi M.;Khalafy, Jabbar. And the article was included in Journal of Heterocyclic Chemistry in 2000.Product Details of 5388-42-1 This article mentions the following:

Conference proceedings containing review material. A comparative study of the flash vacuum pyrolysis of a number of N-alkyl- and N-acylbenzotriazoles and -benzisoxazolones has confirmed that carbene-derived pathways predominate at lower temperatures, and radical pathways at higher temperatures Two new general unimol. thermal reactions are also highlighted. In the experiment, the researchers used many compounds, for example, 2-Phenylisoindolin-1-one (cas: 5388-42-1Product Details of 5388-42-1).

2-Phenylisoindolin-1-one (cas: 5388-42-1) belongs to indole derivatives. Indole could be stereoselectively alkylated with chiral cyclopentyl sulfone reagent. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). Product Details of 5388-42-1

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