Journal
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
Volume 19, Issue -, Pages 231-244Publisher
BEILSTEIN-INSTITUT
DOI: 10.3762/bjoc.19.22
Keywords
C-S; O bond formation; metal -free; oxidative amidation; pyrazole; carbaldehydes; sulfur insertion; thioamides
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An operationally simple and metal-free approach is described for the synthesis of pyrazole-tethered thioamide and amide conjugates. The advantages of this developed protocol refer to the broad substrate scope, metal-free and easy to perform reaction conditions. Moreover, the pyrazole C-3/5-linked amide conjugates were also synthesized via an oxidative amination of pyrazole carbaldehydes and 2-aminopyridines using hydrogen peroxide as an oxidant.
An operationally simple and metal-free approach is described for the synthesis of pyrazole-tethered thioamide and amide conjugates. The thioamides were generated by employing a three-component reaction of diverse pyrazole C-3/4/5 carbaldehydes, secondary amines, and elemental sulfur in a single synthetic operation. The advantages of this developed protocol refer to the broad substrate scope, metal-free and easy to perform reaction conditions. Moreover, the pyrazole C-3/5-linked amide conjugates were also synthesized via an oxidative amination of pyrazole carbaldehydes and 2-aminopyridines using hydrogen peroxide as an oxidant.
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