An efficient, one‐pot synthesis of 2‐deoxy‐2‐[18F]fluoroacetamido‐D‐glucopyranose (N‐[18F]fluoroacetyl‐D‐glucosamine), potential diagnostic imaging agent

Abstract

A rapid, one‐pot synthesis of 2‐deoxy‐2‐[¹⁸F]fluoroacetamido‐D‐glucopyranose (N‐[¹⁸F]fluoroacetyl‐D‐glucosamine) (1) starting from [¹⁸F]fluoride and ethyl bromoacetate is described. The synthesis was accomplished by a combination of halogen exchange, alkaline hydrolysis, and condensation. [¹⁸F]Fluoride was produced by the ¹⁸O (p, n) ¹⁸F nuclear reaction using the cyclotron. The total synthesis time, the radiochemical yield, and purity of (1) are ca. 90 min, ca. 9.1%, and >98%, respectively. Sugar (1) showed the diagnostic tumor‐imaging activity.