Rapid Synthesis of π-Phenylglycine by Carboxylation of π-Lithiobenzylisocyanide

Abstract

An expanding field of interest in nuclear medicine is the preparation of radiopharmaceuticals labelled with cyclorrn produced isotopes of short half life.^1–3 In an investigation to prepare ¹¹C-labelled amino acids we developed a new and repid synthesis for the preparation of a-phenylglycine. The preparation of other amino acids by this route is under investigation. α-Lithiobenzylisocyande⁴ was treated with carbondioxyde and the intermediate was hydrolysed to the amino acid. The overall yield (75–808) was accomplished in 50–70 minutes.⁺