Day: January 4, 2023

Benign One-Pot Synthesis of Carbamo(dithioperoxo)thioate Compounds in Water Medium Using N-(Arylthio)phthalimides as the Electrophilic Sulfur Source was written by Dutta, Soumya;Saha, Amit. And the article was included in ChemistrySelect in 2018.Related Products of 14204-27-4 This article mentions the following:

Carbamo(dithioperoxo)thioate compounds were synthesized in aqueous medium under open aerial condition at room temperature N-(arylthio)phthalimides were used as electrophilic sulfur donors which reacted with in-situ generated dithiocarbamate anions, produced carbamo(dithioperoxo)thioates in excellent yields. After the reaction, phthalimide residue was recovered and reused to prepare N-(arylthio)phthalimides. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Related Products of 14204-27-4).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Related Products of 14204-27-4

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

Effect of hydrogen bonding and solvation of 5-substituted indole carboxldehydes in methanol-benzene was written by Heda, L. C.;Sharma, Rashmi;Chaudhari, Pramod B.. And the article was included in Research Journal of Chemical Sciences in 2011.Name: 5-Chloroindole-3-carboxaldehyde This article mentions the following:

Effect of hydrogen bonding of 5-substituted indole carboxaldehyde was studied by viscometric measurement. The viscosity of the system increases with the increase in concentration The Trend Change Point (TCP) values were determined by intersection of two straight lines, which are dependent on the composition of solvent mixtures The study confirms that the nature of synthesized compounds forms clusters in methanol-benzene mixture The viscometric data were analyzed in terms of Einstein, Vand, Moulik and Jones-Dole equations. These known equations were successfully applied to explain the results of viscosity measurements and the viscometric parameters show that the behavior of compound changes in alc.-benzene. The formation of cluster depends on the methanol concentration The observed methanol concentration effect on the formation of clusters interferences in formation of hydrogen bonding of methanol with mol. In the experiment, the researchers used many compounds, for example, 5-Chloroindole-3-carboxaldehyde (cas: 827-01-0Name: 5-Chloroindole-3-carboxaldehyde).

5-Chloroindole-3-carboxaldehyde (cas: 827-01-0) 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. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Name: 5-Chloroindole-3-carboxaldehyde

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

Microwave promoted and improved thermal synthesis of spiro[indole-pyranobenzopyrans] and spiro[indole-pyranoimidazoles] was written by Dandia, Anshu;Singh, Ruby;Sachdeva, Harshita;Gupta, Rajive;Paul, Satya. And the article was included in Journal of the Chinese Chemical Society (Taipei, Taiwan) in 2003.Category: indole-building-block This article mentions the following:

Spiro[indole-pyranoimidazoles] I (X = 7-NO₂, 5-NO₂, 5-CH₃, 5,7-diCH₃, 5-Br) and spiro[indole-pyranobenzopyrans] II (X = 7-NO₂, 5-NO₂, 5,7-diCH₃, 5-Br, 5-Cl) are readily synthesized in one step in 86-92 and 91-97% yields by the Michael condensation of 3-dicyanomethylene-2H-indol-2-ones III with 1-phenyl-2-thiohydantoin (IV) and 4-hydroxy-2H-1-benzopyran-2-one (V), resp., without using any catalyst under different reaction conditions (conventional heating and microwave irradiation using (a) polar solvent (b) neutral alumina/silica gel as inorganic solid support in solvent free conditions). III was synthesized in situ by the Knoevenagel condensation of indole-2,3-diones and malononitrile in the absence of any catalyst. 100% Conversion was observed in most cases on TLC which also showed the formation of a single product. The comparison between the various methods is established. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Category: indole-building-block).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.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

Nitrosoarene-catalyzed regioselective aromatic C-H sulfinylation with thiols under aerobic conditions was written by Pradhan, Suman;Patel, Sandeep;Chatterjee, Indranil. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2020.Related Products of 4769-96-4 This article mentions the following:

Aromatic amines, e.g. PhX (X = Me₂N, Et₂N, PhNH, morpholin-4-yl, etc.), and (hetero)arenes, such as indoles and pyrroles, were regioselectively sulfinylated using aryl thiols RSH (R = Ph, 4-MeC₆H₄, 4-ClC₆H₄, 2-thienyl, 2-pyridyl, etc.) under mild aerobic conditions using nitrosoarenes as a redox-catalyst to give (arylsulfinyl)amines p-XC₆H₄S(O)R, 3-(arylsulfinyl)indoles and 2-(arylsulfinyl)pyrroles. The nitrosoarene is involved in the electron transfer process with arenes to generate a crucial arene radical cation intermediate for C-H sulfinylation. The present methodol. requires no directing group, could be scaled up easily and is applicable for the late-stage functionalization of drug mols. and natural products with high regioselectivity. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Related Products of 4769-96-4).

6-Nitro-1H-indole (cas: 4769-96-4) 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.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Related Products of 4769-96-4

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

1,2,3-Thiadiazole substituted pyrazolones as potent KDR/VEGFR-2 kinase inhibitors was written by Tripathy, Rabindranath;Ghose, Arup;Singh, Jasbir;Bacon, Edward R.;Angeles, Thelma S.;Yang, Shi X.;Albom, Mark S.;Aimone, Lisa D.;Herman, Joseph L.;Mallamo, John P.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Safety of 1,4-Dimethyl-1H-indole-3-carbaldehyde This article mentions the following:

KDR kinase inhibition is considered to play an important role in regulating angiogenesis, which is vital for the survival and proliferation of tumor cells. Recently we disclosed a structure-based kinase inhibitor design strategy which led to the identification of a new class of VEGFR-2/KDR kinase inhibitors bearing heterocyclic substituted pyrazolones as the core template. Instability in a rat S9 preparation and poor iv PK profiles for most of these inhibitors necessitated exploration of new pyrazolones to identify new analogs with improved metabolic stability. Optimization of the heterocyclic moiety led to the identification of the thiadiazole series of pyrazolones (D) as potent VEGFR-2/KDR kinase inhibitors. SAR modifications, kinase selectivity profiling, and structural elements for improved PK properties were explored. Oral bioavailability up to 29% was achieved in the rat. Modeling results based on the Glide XP docking approach supported our postulation regarding the interaction of the lactam segment of the pyrazolones with the hinge region of the KDR kinase. In the experiment, the researchers used many compounds, for example, 1,4-Dimethyl-1H-indole-3-carbaldehyde (cas: 170489-16-4Safety of 1,4-Dimethyl-1H-indole-3-carbaldehyde).

1,4-Dimethyl-1H-indole-3-carbaldehyde (cas: 170489-16-4) 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. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Safety of 1,4-Dimethyl-1H-indole-3-carbaldehyde

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

Metal-organic framework MIL-53(Al): synthesis, catalytic performance for the Friedel-Crafts acylation, and reaction mechanism was written by Yan, Junlei;Jiang, Sai;Ji, Shengfu;Shi, Da;Cheng, Hefei. And the article was included in Science China: Chemistry in 2015.Quality Control of 6-Nitro-1H-indole This article mentions the following:

Metal-organic framework MIL-53(Al) was synthesized by a solvothermal method using aluminum nitrate as the aluminum source and 1,4-benzenedicarboxylic acid (H2BDC) as the organic ligand. The structure of samples was characterized by X-ray diffraction (XRD) and Fourier transform IR spectroscopy (FT-IR). The catalytic activity and recyclability of MIL-53(Al) catalyst for the Friedel-Crafts acylation reaction of indole with benzoyl chloride were evaluated. The reaction conditions were optimized and a reaction mechanism was suggested. The results showed that the MIL-53(Al) catalyst exhibited good catalytic activity and recyclability for the Friedel-Crafts acylation reaction. When the molar ratio of indole and MIL-53(Al) catalyst was 1:0.06 (n₁:n _catalyst), the molar ratio of indole and benzoyl chloride was 1:3, and the solvent was dichloromethane, the conversion of indole could reach 97.1% and the selectivity of 3-acylindole could reach 81.1% at 25 °C after 8 h. The catalyst can be reused without significant degradation in catalytic activity. After the catalyst was reused five times, the conversion of indole was 87.6% and the selectivity of 3-acylindole was 79.5%. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Quality Control of 6-Nitro-1H-indole).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole exists overwhelmingly in the 1H-indole form as do other simple indoles. 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). Quality Control of 6-Nitro-1H-indole

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-Catalyzed Direct and Specific C-7 Acylation of Indolines with 1,2-Diketones was written by Xie, Guilin;Zhao, Yuhan;Cai, Changqun;Deng, Guo-Jun;Gong, Hang. And the article was included in Organic Letters in 2021.HPLC of Formula: 4769-96-4 This article mentions the following:

Herein, a palladium-catalyzed direct and specific C-7 acylation of indolines in the presence of an easily removed directing group was developed. This strategy usually considered as a practical strategy for the preparation of acylated indoles because indoline can be easily converted to indole under oxidation conditions. In particular, these strategy greatly improved the alkacylation yield of indolines for which only an unsatisfactory yield could be achieved in the previous studies. Furthermore, the reaction can be scaled up to gram level in the standard reaction conditions with a much lower palladium loading (1 mol %). In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4HPLC of Formula: 4769-96-4).

6-Nitro-1H-indole (cas: 4769-96-4) 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. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.HPLC of Formula: 4769-96-4

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

Dehydrogenation of Nitrogen Heterocycles Using Graphene Oxide as a Versatile Metal-Free Catalyst under Air was written by Zhang, Jingyu;Chen, Shiya;Chen, Fangfang;Xu, Wensheng;Deng, Guo-Jun;Gong, Hang. And the article was included in Advanced Synthesis & Catalysis in 2017.HPLC of Formula: 4769-96-4 This article mentions the following:

Graphene oxide (GO) has been developed as an inexpensive, environmental friendly, metal-free carbocatalyst for the dehydrogenation of nitrogen heterocycles. Valuable compounds, such as quinoline, 3,4-dihydroisoquinoline, quinazoline, and indole derivatives, have been successfully used as substrates. The investigation of various oxygen-containing mols. with different conjugated systems indicated that both the oxygen-containing groups and large π-conjugated system in GO sheets are essential for this reaction. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4HPLC of Formula: 4769-96-4).

6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole produced by Proteus, Pseudomonas, Escherichia and other species was shown to be a growth promoting factor in Arabidopsis thaliana. 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). HPLC of Formula: 4769-96-4

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, characterization and evaluation of antioxidant activity of N-([1,3,4]oxadiazino[6,5-b] substituted indol-3-ylmethyl)aniline was written by Padma, Bairy;Gadea, Sammaiah. And the article was included in Pharma Innovation in 2020.Computed Properties of C8H4N2O4 This article mentions the following:

A novel series of N-([1,3,4]oxadiazino[6,5-b] substituted indol-3-ylmethyl)anilines I [R = H, 5-Me, 7-Br, etc.] were synthesized in good yields and characterized by IR, NMR and mass spectral analyses. Synthesized compounds I were evaluated for their antioxidant activity by standard DPPH assay method. By taking ascorbic acid as standard drug, among the series the compounds I [R = 7-Cl, 5-COOEt, 7-OH] were potent antioxidant and remaining compounds showed significant antioxidant activity. In the experiment, the researchers used many compounds, for example, 7-Nitroindoline-2,3-dione (cas: 112656-95-8Computed Properties of C8H4N2O4).

7-Nitroindoline-2,3-dione (cas: 112656-95-8) 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. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Computed Properties of C8H4N2O4

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 First Bioreversible Prodrug of Metformin with Improved Lipophilicity and Enhanced Intestinal Absorption was written by Huttunen, Kristiina M.;Mannila, Anne;Laine, Krista;Kemppainen, Eeva;Leppanen, Jukka;Vepsalainen, Jouko;Jarvinen, Tomi;Rautio, Jarkko. And the article was included in Journal of Medicinal Chemistry in 2009.Recommanded Product: 14204-27-4 This article mentions the following:

Metformin is a potent antidiabetic agent and currently used as a first-line treatment for patients with type 2 diabetes. Unfortunately, the moderate absorption and uncomfortable gastrointestinal adverse effects associated with metformin therapy impair its use. In this study, two novel prodrugs of a biguanidine functionality containing antidiabetic agent, metformin, were designed, synthesized, and evaluated in vitro and in vivo to accomplish improved lipophilicity and, consequently, enhanced oral absorption of this highly water-soluble drug. These results represent that the more lipophilic prodrug 2a biotransformed quant. to metformin mainly after absorption. The enhanced oral absorption consequently promoted the bioavailability of metformin from 43% to 65% in rats. Thus, this novel prodrug may offer a solution to reduce the required daily doses of metformin, which may decrease the uncomfortable adverse effects associated with metformin therapy. In the experiment, the researchers used many compounds, for example, 2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4Recommanded Product: 14204-27-4).

2-(Phenylthio)isoindoline-1,3-dione (cas: 14204-27-4) 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. 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). Recommanded Product: 14204-27-4

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