What is it about?
Efficient approach based on Pfitzinger reaction of 5-sulfonylated isatins with a mixture of ethyl 4-chloro-3-oxo-butanoate and morpholine, was developed to synthesize novel 4,8-disubstituted derivatives of 1,3-dihydropyrrolo[3,4-c]quinoline-l,3-diones, which represent a valuable pharmacophore chemotype.
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Why is it important?
The synthetic approach allows for design and high throughput synthesis of combinatorial libraries of potential Caspase 3 inhibitors
Perspectives
Search for new drugs in different areas of human diseases is often bootstrapped by complicated chemistry. Developing simpler synthetic approaches that allow for creation of small molecule libraries in high throughput fashion, substantially increases probabilities of finding new target specific drug candidates with improved pharmacokinetic, pharmacodynamic, and low toxicity parameters.
Dr. ILYA OKUN
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This page is a summary of: NEW VARIANT OF THE PEIZINGER REACTION. SYNTHESIS AND CHEMICAL TRANSFORMATIONS OF SUBSTITUTED 2-AMINOMETHYL-QUINOLINE-3,4-DICARBOXYLIC ACIDS, Heterocyclic Communications, January 2006, De Gruyter,
DOI: 10.1515/hc.2006.12.1.15.
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