1560948-53-9

Upstream product

• 610-94-6 2-bromobenzoic acid methyl ester 
• 3034-86-4 4-ethynylbenzoic acid methyl ester 
• 1425605-52-2 methyl 4-((2-carbamoylphenyl)ethynyl)benzoate 
• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 124394-21-4 3-(4-bromophenyl)isoquinolin-1(2H)-one 
• 118520-88-0 3-(4-bromophenyl)-1H-2-benzopyran-1-one 
• 118520-73-3 2-(4-bromophenylethynyl)benzoic acid methyl ester 
• 766-96-1 4-bromo-1-ethynylbenzene 
• 610-97-9 o-iodo-methyl-benzoic acid 

Downstream Products

• 1560948-66-4 3-(4-hydroxymethylphenyl)-2H-isoquinolin-1-one 
• 1560948-76-6 3-[4-(1-fluoro-1-methylethyl)phenyl]-2H-isoquinolin-1-one 
• 1560948-55-1 3-[4-(1-hydroxy-1-methylethyl)phenyl]-2H-isoquinolin-1-one 

Relevant academic research and scientific papers

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.

Triflic acid mediated sequential cyclization of ortho-alkynylarylesters with ammonium acetate

A triflic acid (TfOH) mediated sequential cyclization of ortho-alkynylarylesters and ammonium acetate (NH4OAc) was reported. The reaction took place via a Br?nsted acid-mediated intramolecular cyclization of ortho-alkynylarylesters followed by an ammonium acetate participated substitution reaction, forming isoquinolin-1-ones as the major products. Different from most of the known synthetic methods of isoquinolin-1-ones, no metal catalyst was required in the reported reaction. The regioisomers – isoindolin-1-ones were obtained together with isoquinolin-1-ones in a few cases. The intermediate compounds – isochromen-1-ones and isobenzofuran-1-ones were also isolated. The interconversion experiments showed that the regioisomers formed during the Br?nsted acid induced intramolecular cyclization of ortho-alkynylarylesters. A natural product – ruprechstyril was prepared in a moderate yield employing the new method.

(AZA-)ISOQUINOLINONE DERIVATIVES

Compounds of the formula (I), in which R1, X, Y and n have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.