1094019-47-2

Upstream product

• 135030-39-6 3-(4-fluorophenyl)-1H-2-benzopyran-1-one 
• 1260150-34-2 1-ethoxy-3-(4-fluorophenyl)isoquinoline 
• 5597-04-6 2-cyanomethylbenzoic acid methyl ester 
• 1765-93-1 4-fluoroboronic acid 
• 2042-37-7 o-cyanobromobenzene 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 3930-83-4 o-iodobenzamide 
• 4001-73-4 2-Bromobenzamide 

Relevant academic research and scientific papers

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

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.

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.

Synthetic method of antitumor nitrogen-containing heterocyclic drug intermediates

The invention relates to a synthetic method of isoquinolinone compounds shown by formula (III) shown in the description and acting as antitumor nitrogen-containing heterocyclic drug intermediates; the method comprises: enabling a compound of formula (I) shown in the description and a compound of formula (II) shown in the description to react in a reaction solvent in the presence of a catalyst, a nitrogen-containing ligand and an acid catalyst, and treating after reaction to obtain the compound of formula (III), wherein R1 is C1-C6 alkyl, and R2 is H, halogen, C1-C6 alkyl or C1-C6 alkoxy, or R2 and R2-substituted phenyl form naphthyl. Through the comprehensive selection and interaction of a reaction substrate, catalysts, nitrogen-containing ligands, acid catalysts, reaction solvents and the like according to the method, the substrate range is widened, and the isoquinolinone compound is acquired at high yield; more diversified intermediates are provided for novel synthesis of the compounds and the research, development and synthesis of antitumor drugs, and the compounds have good research value and application potential.

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

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.

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

Platinum(II)-catalyzed intramolecular cyclization of alkynylbenzonitriles: Synthesis of 1-alkoxyisoquinolines and isoquinolones

A facile synthesis of a series of 1-alkoxyisoquinolines and (2H)-isoquinolones by an intramolecular 6-endo-dig cyclization of ortho-alkynylbenzonitriles in the presence of a catalytic amount of hydrido(dimethylphosphinous acid-κP)[hydrogen bis(dimethylphosphinito- κP)]platinum(II) in various alcohols at 65-90 °C is described for the first time.

Efficient synthesis of some 3-arylisoquinolin-1(2H)-ones

A number of 3-arylisoquinolin-1(2H)-ones were efficiently prepared from the corresponding 3-aryl-isocoumarins by refluxing with methanamide.