18029-60-2

Upstream product

• 1211580-83-4 4-bromo-6,7-dimethoxyisoquinolin-1(2H)-one 
• 96729-80-5 2-(3,4-dimethoxyphenyl)-3-oxopropanenitrile 
• 51-79-6 urethane 
• 93-17-4 3,4-dimethoxyphenylacetonitrile 
• 18029-59-9 ethyl (2-cyano-2-(3,4-dimethoxyphenyl)vinyl)carbamate 

Downstream Products

• 798565-60-3 C₂₁H₁₉N₅O₄ 
• 798565-62-5 1-(3-ethoxy-benzoyl)-6,7-dimethoxy-isoquinoline-4-carbonitrile 
• 798565-60-3 [6,7-dimethoxy-4-(1H-tetrazol-5-yl)-isoquinolin-1-yl]-(3-ethoxy-phenyl)-methanone 
• 798565-73-8 1-(3-ethoxy-benzoyl)-6,7-dimethoxy-isoquinoline-4-carboxylic acid amide hydrochloride 
• 798565-46-5 6,7-dimethoxy-1-(3-methylsulfanyl-benzoyl)-isoquinoline-4-carbonitrile 
• 798566-03-7 1-(3-hydroxyethoxy-benzoyl)-6,7-dimethoxy-isoquinoline-4-carbonitrile 

Relevant academic research and scientific papers

Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors

Through high throughput screening and subsequent hit identification and optimization, we synthesized a series of 1-arylcarbonyl-6,7- dimethoxyisoquinoline derivatives as the first reported potent and reversible GFAT inhibitors. SAR studies of this class o

Strategies and synthetic methods directed toward the preparation of libraries of substituted isoquinolines

Strategies for the production of substituted isoquinoline libraries were developed and explored. Routes involving microwave-assisted variants of the Bischler-Napieralski or Pictet-Spengler reaction allowed for cyclization of substituted β-arylethylamine derivatives. The dihydroisoquinolines and tetrahydroisoquinolines thus generated could then be oxidized to their corresponding isoquinoline analogues. An alternate strategy, however, involving the preparation and activation of isoquinolin-1(2H)-ones is demonstrated to be a more practical, rapid, and efficient route to C1- and C4-substituted isoquinoline libraries.

GLUTAMINE FRUCTOSE-6-PHOSPHATE AMIDOTRANSFERASE (GFAT) INHIBITORS

Compounds of formula (I) are provided, wherein R1 and R2 are as designated in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.

GFAT INHIBITORS

Compounds of formula (I) are provided as well as pharmaceutically acceptable salts and esters thereof, wherein the substituents are as disclosed in the specification. The compounds have utility for the treatment of type 2 diabetes mellitus.