75040-00-5

Upstream product

• 124394-17-8 2-(p-tolylethynyl)benzamide 
• 6639-19-6 N,N,2-trimethylbenzamide 
• 104-85-8 para-methylbenzonitrile 
• 253435-24-4 2-(2-(4-(methyl)phenyl)ethynyl)benzonitrile 
• 2170-09-4 N,2-dimethylbenzamide 
• 89641-06-5 2-iodo benzoyl azide 
• 766-97-2 4-n-methylphenylacetylene 
• 2042-37-7 o-cyanobromobenzene 
• 122-00-9 para-methylacetophenone 
• 5597-04-6 2-cyanomethylbenzoic acid methyl ester 
• 5720-05-8 4-methylphenylboronic acid 
• 55-21-0 benzamide 
• 1821-34-7 N-chlorobenzamide 
• 88-67-5 2-Iodobenzoic acid 

Downstream Products

• 194292-30-3 1-chloro-3-p-tolyl-isoquinoline 

Relevant academic research and scientific papers

Nickel-Catalyzed Tandem Reaction of Functionalized Arylacetonitriles with Arylboronic Acids in 2-MeTHF: Eco-Friendly Synthesis of Aminoisoquinolines and Isoquinolones

The first example of the nickel-catalyzed tandem addition/cyclization of 2-(cyanomethyl)benzonitriles with arylboronic acids in 2-MeTHF has been developed, which provides the facile synthesis of aminoisoquinolines with good functional group tolerance under mild conditions. This chemistry has also been successfully applied to the synthesis of isoquinolones by the tandem reaction of methyl 2-(cyanomethyl)benzoates with arylboronic acids. The use of the bio-based and green solvent 2-MeTHF as the reaction medium makes the synthesis process environmentally benign. The synthetic utility of this chemistry is also indicated by the synthesis of biologically active molecules.

Tandem addition/cyclization for access to isoquinolines and isoquinolones via catalytic carbopalladation of nitriles

The first example of the palladium-catalyzed sequential nucleophilic addition followed by an intramolecular cyclization of functionalized nitriles with arylboronic acids has been achieved, providing an efficient synthetic pathway to access structurally di

Direct access to cobaltacycles via C-H activation: N-chloroamide- enabled room-temperature synthesis of heterocycles

Cobaltacycle synthesis via C-H activation has been achieved for the first time, providing key mechanistic insight into cobalt catalytic chemistry. NChloroamides are used as a directing synthon for cobalt-catalyzed roomtemperature C-H activation and construction of heterocycles. Alkynes as coupling partners allow convenient access to isoquinolones, a class of synthetically and pharmaceutically important compounds. The broad substrate scope enables a diverse range of substitution patterns to be incorporated into the heterocyclic scaffold.

On-Water Silver(I)-Catalyzed Cycloisomerization of Acetylenic Free Amines/Amides towards 7-Azaindole/Indole/Isoquinolone Derivatives

Silver-catalyzed on-water intramolecular cyclization of acetylenic free amines is reported, which affords 7-azaindoles in good to excellent yields. Neither strong base/acid catalysts nor N-substituted substrates are required to achieve this cycloisomerization. Hydrogen bonds between water medium and the substrates play an important role in improving chemical reactivity and regioselectivity. Furthermore, the on-water reaction is extendable to acetylenic amides for isoquinolone synthesis.

Method for synthesizing anti-cancer inhibitor intermediate

The invention relates to a method for synthesizing an isoquinolone derivative of formula (III) as an anti-cancer inhibitor intermediate. The method comprises the step: in a reaction solvent, in the presence of a catalyst, a nitrogen-containing ligand, an acid additive and 4-dimehtyl aminopyridine, performing a reaction on a compound of formula (I) as shown in the specification and a compound of formula (II) as shown in the specification, and after posttreatment, obtaining a compound of formula (III) as shown in the specification, wherein in the formulae, R1 is C1-C6 alkyl; R2 is H, halogen, C1-C6 alkyl or C1-C6 alkoxy; or R2 and substituted phenyl form naphthyl; and M is an alkali metal element. By adopting the method, due to comprehensive selection and mutual action of a reaction substrate, the catalyst, the nitrogen-containing ligand, the acid additive, the 4-dimehtyl aminopyridine and the solvent, the substrate range can be widened, a target product of high yield can be obtained, an intermediate of relatively rich diversities can be provided for synthesis of the compounds and development and synthesis of anti-cancer inhibitor medicines, and good research values and application potential can be achieved.

A different quinolinone and its derivatives

The invention belongs to the technical field of pharmaceutical and chemical intermediates and related chemicals and relates to a preparation method of isoquinolone and derivatives thereof. The isoquinolone and derivatives thereof are important biologically active molecules, skeletal structures frequently appear in natural molecules and drug molecules, and have better therapeutic effect on hypertension, cancer and anxiety disorders and important applications in the fields of organic synthesis and pharmaceutical chemistry. The method is short in synthesis route, mild in conditions and simple in operation and is expected to achieve industrial production and has the advantages of short synthetic route, mild conditions, simple operation and high yield and the like. The isoquinolone and derivatives thereof have greater application value and social and economic benefits.

Isoquinolone synthesis through SNAr reaction of 2-halobenzonitriles with ketones followed by cyclization

An efficient method for the synthesis of isoquinolones through base KOtBu-promoted SNAr reaction of 2-halobenzonitriles with ketones followed by Lewis acid Cu(OAc)2-catalyzed cyclization is described. Isoquinolone derivati

A simple access to N-(un)substituted isoquinolin-1(2H)-ones: Unusual formation of regioisomeric isoquinolin-1(4H)-ones

A ligand/additive/Pd-free Cu-mediated coupling/cyclization strategy afforded the first practical, one-pot and general approach towards synthesis of N-(un)substituted isoquinolin-1(2H)-ones. Both the catalyst and the solvent used are recyclable. The use of the Cu reagent in excess led to the unusual formation of regioisomeric and uncommon isoquinolin-1(4H)-ones. This journal is the Partner Organisations 2014.

Copper-catalyzed selective synthesis of isoindolin-1-ones and isoquinolin-1-ones from the three-component coupling of 2-halobenzoic acid, alkynylcarboxylic acid and ammonium acetate

Isoindolin-1-ones and isoquinolin-1-ones were selectively synthesized from the reaction of 2-halobenzoic acid, arylalkynylcarboxylic acid and ammonium acetate (NH4OAc) in the presence of cesium carbonate (Cs2CO3) and a copper catalyst. Conducting the reaction under one-pot conditions provided isoindolin-1-ones in good yields. Changing the addition sequence of ammonium acetate after all reagents had reacted at 120 °C for 6 h selectively produced isoquinolin-1-ones. A variety of arylalkynylcarboxylic acids produced the corresponding isoindolin-1-ones and isoquinolin-1-ones in good yields.

Synthesis of functionalized isoquinolin-1(2H)-ones by copper-catalyzed α-arylation of ketones with 2-halobenzamides

Copper is key: A concise route to isoquinolin-1(2H)-ones from simple and readily available starting materials is provided by an efficient copper-catalyzed annulation of ketones with 2-halobenzamides. The method is applicable to a wide range of ketones con