Synthesis of β‐Fluorophenethyl Halopyridyl Thiourea Compounds as Non‐nucleoside Inhibitors of HIV‐1 Reverse Transcriptase

Abstract

Synthesis of β‐fluorophenethylamines was accomplished in three steps with an overall yield of 50%. Condensation of β‐fluorophenethylamine hydrochloride with thiocarbonylimidazole derivative derived from halopyridyl amines in dimethylformamide furnished the desired thiourea compounds as crystalline solids. Several of the β‐fluorophenethyl thiourea compounds inhibited HIV‐1 reverse transcriptase (RT) at nanomolar to low micromolar concentrations.

Keywords:

• β‐Fluorophenethylamines
• Thiourea
• HIV‐1
• Reverse transcriptase