The synthesis of [4‐3H]oxiracetam ‐ a novel nootropic agent

Abstract

AbstractThe synthesis of [4‐3H]oxiracetam (6) from ethyl 2‐(4‐chloro‐3‐oxo‐butyramido)acetate (1) is described. Ethyl 2‐(4‐chloro‐3‐oxo‐butyramido)‐acetate (1) was reduced with sodium borotritide at Amersham International plc (TR5 tritiation service) to give ethyl 2‐(4‐chloro‐[3‐3H]‐3‐hydroxy‐butyramido)acetate (2). This was elaborated, in four steps, to [4‐3H] oxiracetam (6) in 4.8% overall radiochemical yield, furnishing 5735 μCi, 212 MBq, 41.8 μg, of specific activity 21.7 Ci/mmol, 802.9 GBq/mmol, and radiochemical purity of greater than 98%.