NIS-promoted guanylation of amines

An efficient NIS-promoted guanylation reaction is described. This procedure allows the guanylation of primary and secondary amines through the reaction with di-Boc-thiourea and di-Boc- S-methylisothiourea, respectively. We demonstrated that the use of NIS compares favorably with existing methods and...

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Veröffentlicht in:Tetrahedron letters 2009-04, Vol.50 (13), p.1463-1465
Hauptverfasser: Ohara, Keiichiro, Vasseur, Jean-Jacques, Smietana, Michael
Format: Artikel
Sprache:eng
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Zusammenfassung:An efficient NIS-promoted guanylation reaction is described. This procedure allows the guanylation of primary and secondary amines through the reaction with di-Boc-thiourea and di-Boc- S-methylisothiourea, respectively. We demonstrated that the use of NIS compares favorably with existing methods and is an attractive alternative to heavy metal or Mukayama’s reagent activation.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2009.01.073