4.1 Article

H3PO4 catalyzed one-pot synthesis of 1,3-diphenyl-1H-pyrazole-4-carbaldehyde to novel 1,3-diphenyl-1H-pyrazole-4-carbonitrile

Journal

JOURNAL OF CHEMICAL SCIENCES
Volume 133, Issue 3, Pages -

Publisher

INDIAN ACAD SCIENCES
DOI: 10.1007/s12039-021-01939-w

Keywords

Pyrazole-4-carbaldehyde; pyrazole-4-carbonitrile; H3PO4; formic acid

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By utilizing formic acid as a medium, one-pot condensation of pyrazole-4-aldehydes and hydroxylamine hydrochloride, followed by dehydration with a catalytic amount of orthophosphoric acid, leads to the formation of novel pyrazole-4-carbonitrile. This metal-free and cost-effective method yields excellent results and provides a versatile precursor for the synthesis of various valuable compounds.
One-pot condensation of pyrazole-4-aldehydes and hydroxylamine hydrochloride to form the corresponding oxime using formic acid as a medium and further dehydration of oxime using a catalytic amount of orthophosphoric acid to afford novel pyrazole-4-carbonitrile. This protocol serves as an ortho-phosphoric acid-catalyzed one-pot conversion of aldehyde to nitrile. Most remarkable features of this method are metal-free, cost-effective, atom efficiency with excellent yield (98-99%). This process will serve as a robust and scalable tool for the synthesis of valuable and versatile precursor (nitriles). This precursor will pave the way for the synthesis of various medicinally important valuable compounds. Graphic abstract H3PO4 catalysed transformation of aldehydes to nitriles

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