121491-39-2

Upstream product

• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 71727-37-2 2-phenyl-pyrazolo[1,5-a]pyridine-3-carbaldehyde 
• 56983-95-0 2-phenylpyrazolo[1,5-a]pyridine 
• 1117-37-9 ethyl (E)-3-(dimethylamino)acrylate 
• 5443-49-2 α-bromocinnamaldehyde 
• 66894-04-0 2,3-dibromo-3-phenyl propanal 
• 14371-10-9 (E)-3-phenylpropenal 
• 2579-22-8 Phenylpropargyl aldehyde 
• 6295-87-0 N-aminopyridin-1-ium iodide 
• 117552-48-4 E-5-phenyl-pent-2-en-4-ynoic acid ethyl ester 
• 131073-06-8 triethyl phosphonoacetate 
• 340771-05-3 2-Phenyl-pyrazolo[1,5-a]pyridine-4-carboxylic acid ethyl ester 

Downstream Products

• 121524-18-3 (2R)-1-[3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)acryloyl]-2-(2-hydroxyethyl)piperidine 
• 137453-39-5 3-(2-phenylpyrazolo[1,5-a]-pyridin-3-yl)acrylic acid 

Relevant academic research and scientific papers

Process development of a novel non-xanthine adenosine A1 receptor antagonist

(+)-(R)-1-[(E)-3-(2-phenylpyrazolo[l,5-a]pyridin-3-yl)acryloyl]-2- piperidine ethanol (FK453) is a novel, potent adenosine AI receptor antagonist for the regulation of renal function. The development of a reliable process suitable for large scale manufacture is described. A Horner-Emmons reaction and a 1,3-dipolar cycloaddition were successfully scaled up to afford ethyl (E)-3-(2-phenylpyrazolo[l,5-a]pyridin-3-yl)acryloylate, with excellent regioselectivity and stereoselectivity. Process improvements and optimization of each step permitted elimination of column chromatography, resulting in a straightforward, practical synthesis of FK453.

Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist

Novel 2-phenylpyrazolo[1,5-a]pyridine-3-acryloylamides were synthesized and evaluated for diuretic activities. FK453 (1d), the most potent compound in this series, was found to be a potent and selective adenosine A1 receptor antagonist, whereas 1e, the (S)-enantiomer of FK453, was a weak and non-selective adenosine antagonist.

Method of treating kidney disease using pyrazolopyridine compound

The invention relates to a method for the treatment of renal toxicity, nephrosis or nephritis which comprises administering an effective amount of the pyrazolopyridine compounds of the invention.

Pharmaceutical method of treatment using pyrazolopyridine compound

The invention relates to a method for the treatment of ailments which comprises administering an effective amount of the pyrazolopyridine compounds of the invention.

Pyrazolopyridine compound and processes for preparation thereof

The disclosure deals with pyrazolopyridine compounds of the formula STR1 wherein the variables are defined in the specification. The compounds are useful in the treatment of bronchial asthma, immunosuppression, diabetes, etc.

Pharmaceutically useful pyrazolopyridines

The disclosure deals with a pyrazolopyridine compound of the formula STR1 wherein the variables are defined in the specification. The compounds are useful as a diuretic, antihypertensive agent, etc.