Temperature-Controlled Thiation of α-Cyano-ß-Alkynyl Carbonyl Derivatives for De Novo Synthesis of 2-Aminothiophenes and Thieno[2,3- c]isothiazoles.
J Org Chem
; 83(23): 14688-14697, 2018 12 07.
Article
em En
| MEDLINE
| ID: mdl-30277073
ABSTRACT
Making use of temperature-controlled thiation as a key operation, a simple route to 2-aminothiophenes or thieno[2,3- c]isothiazoles has been newly developed wherein the 2-aminothiophene nucleus was formed through an initial formation of thioamide followed by a 5-exo-dig addition to the tethered alkyne; however, under harsher thermal conditions, excess sulfur-transferring reagents enabled further oxidative thiation to generate the corresponding thieno[2,3- c]isothiazoles.
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MEDLINE
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Ano de publicação:
2018
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Article