39830-75-6

Upstream product

• 16800-68-3 1-acetyl-2,3-dihydro-1H-indol-3-one 
• 100-52-7 benzaldehyde 
• 201230-82-2 carbon monoxide 
• 615-43-0 2-iodophenylamine 
• 536-74-3 phenylacetylene 
• 2258-42-6 formyl acetic anhydride 
• 3260-61-5 indolin-3-one 
• 124857-13-2 1-(2-Aminophenyl)-3-phenyl-2-propyn-1-one 
• 124-38-9 carbon dioxide 
• 132114-99-9 (E)-1-acetyl-2-benzylideneindolin-3-one 
• 95542-12-4 1-acetyl-2-benzylideneindolin-3-one 
• 97583-87-4 2-amino-4-phenyl-5-acetyl-3-cyano-4H-pyrano<3,2-b>indole 

Downstream Products

• 479-41-4 indirubin 

Relevant academic research and scientific papers

Design, synthesis and characterization of functionalized pyrazole derivatives bearing amide and sulfonamide moieties from aza-aurones

Abstract: In this work, we report the synthesis of new pyrazole derivatives bearing amide and sulfonamide frameworks from aza-aurones. Firstly, the intermediate spiropyrazolines were obtained through a highly regioselective 1,3-dipolar cycloaddition of nitrilimines with aza-aurones. Subsequently, the obtained cycloadducts were subjected to hydrochloric acid in hot ethanol which conducts to 5-(2-aminobenzoyl)-3,4-diaryl-1-phenylpyrazoles. Finally, the target compounds were obtained separately by the action of acetic anhydride, benzoyl chloride and tosyl chloride on the intermediates 2-aminobenzoylpyrazoles, respectively. Structures of all the synthesized compounds were established using IR, 1H NMR and 13C NMR and mass spectroscopy. Graphic Abstract: Synthesis and characterization of novel heterocyclic systems encompassing pyrazole derivatives from aza-aurones are reported. The synthetic routes used in this work are efficient and relevant, involving the 1,3-dipolar cycloaddition and alkylation reactions. The outcomes show that spectroscopic data fit the structure of all synthesized compounds.[Figure not available: see fulltext.]

One-Pot Palladium-Catalyzed Carbonylative Sonogashira Coupling using Carbon Dioxide as Carbonyl Source

Carbonylation coupling reaction has emerged as a powerful and versatile strategy for the construction of carbonyl-containing compounds in modern synthetic chemistry over the past years. Carbon dioxide, a renewable one carbon molecule, has become one of the most attractive and promising alternative carbonyl sources due to its highly abundance, nontoxicity and stability in comparison with CO in recent years. However, in most cases, a two-chamber technique was generally necessary to allow the CO-producing and CO-consuming processes to perform successfully because of the complexities and incompatibility of reaction conditions, when carbon dioxide was utilized as carbonyl source. Herein, a practical one-pot protocol using carbon dioxide as the carbonyl source for the palladium-catalyzed carbonylative Sonogashira coupling has been established, providing an expedient and practical route to a wide range of functionalized alkynones and indoxyls under mild reaction conditions. By finding a suitable catalytic system, the method allowed the CO-generating and CO-consuming processes to proceed in one pot, wherein carbon monoxide was generated in situ from the reduction of carbon dioxide in the absence of any fluoride reagents. Simple and safe operation, readily available substrates, good functional group tolerance and mild reaction conditions are the features of the method.

Indirubin derivative used in combination with polypeptide as well as preparation method and application of indirubin derivative

The invention relates to an indirubin derivative used in combination with polypeptide as well as a preparation method and application of the indirubin derivative, and belongs to the technical field ofmedicinal chemistry. The structure of the compound is shown as a general formula I. The indirubin derivative provided by the invention has an obvious inhibition effect on leukemia cells K562, and theinhibition strength on tumor cells is remarkably improved after the indirubin derivative is combined with polypeptide drug blue peptide. The compound as shown in the general formula I can be appliedto preparation of drugs for treating leukemia or lead compounds developed as drugs for treating leukemia, or used for preparing drugs for treating leukemia and combined with polypeptide drugs.

Lenalidomide derivative capable of inhibiting IDO1 activity as well as preparation method and application of lenalidomide derivative

The invention relates to a lenalidomide derivative capable of inhibiting IDO1 activity as well as a preparation method and application of the lenalidomide derivative, and belongs to the technical field of medicinal chemistry. The structure of the compound is shown as a general formula I. The activity inhibition effect of the lenalidomide derivative provided by the invention on IDO1 is obviously superior to that of indirubin, lenalidomide and pomalidomide. The compound shown in the general formula I can be applied to preparation of drugs for inhibiting the activity of IDO1.

AURONES AND METHODS OF USING AURONES TO TREAT TUBERCULOSIS

This disclosure describes compounds, compositions, and methods for treating or preventing infection or disease including, in some specific embodiments, treating or preventing tuberculosis and/or infection with Mycobacterium tuberculosis (Mtb). In one aspect, this disclosure describes aurones including, for example, aurone 9504, aurone 9505, aurone 9501, aurone 9510, aurone AA2A, and aurone AA8, compositions including aurones, and methods of using aurones for treating or preventing tuberculosis.

A general and convenient palladium-catalyzed synthesis of benzylideneindolin-3-ones with formic acid as the CO source

A general and convenient palladium-catalyzed carbonylative synthesis of 2-benzylideneindolin-3-ones from 2-iodoanilines and arylacetylenes has been developed. With formic acid as the CO source and Ac2O as the activator, a variety of 2-benzylideneindolin-3-ones were obtained in good to excellent yields with exceptional functional group tolerance.

Heterogeneous metallo-organocatalysis for the selective one-pot synthesis of 2-benzylidene-indoxyl and 2-phenyl-4-quinolone

One-pot tandem heterogeneously catalyzed procedures for the selective synthesis of 2-benzylidene-indoxyl and 2-phenyl-4-quinolone have been developed. For this purpose, heterogeneous palladium-, amine-, and phosphine-catalysts were prepared by post-synthe

Color and Constitution. Part 8 . Some Novel Dyestuffs Containing Indoxyl Residues

Novel dyes containing C-linked indoxyl residues are prepared by two routes: (a) by the reaction of C-electrophiles with N-acetylindoxyl and (b) by the reaction of active methylene compounds with 2-chloroindole-3-one.The visible absorption spectra are recorded and discussed.

NEW METHOD OF SYNTHESIS OF δ-CARBOLINES FROM 3-INDOLINONE VIA PYRANOINDOLES

2-Arylidene-1-acetylindolin-3-ones were obtained from 1-acetylindolin-3-ones and p-substituted benzaldehydes or 4-pyridinecarboxaldehyde, by the action of malonodinitrile, and were converted into 2-amino-4-aryl-5-acetyl-3-cyanopyranoindoles.When heated with an aqueous-alcoholic solution of KOH, the latter compounds transform into 2-alkoxy-4-aryl-3-cyano-δ-carbolines.The possible paths of formation of δ-carbolines and pyranoindoles are discussed.