Synthesis of Heterocyclic Thiourea Compounds with Amino Acid Side Chain as Nonnucleoside Inhibitors of HIV‐1 Reverse Transcriptase

Abstract

Heterocyclic thioureas having an amino acid ester side chain were prepared in two steps with overall yields of 65–85%. Condensation of a substituted heterocyclic amine with thiocarbonyldiimidazole, followed by treatment with an amino acid methyl ester hydrochloride in DMF, yielded the desired heterocyclic thioureas as crystalline solids. Amino acid esters such as glycine, leucine, valine, phenyl alanine, and tryptophan were used to prepare these thioureas.

Keywords:

• Thiourea
• amino acid
• heterocyclic
• nonnucleoside