Synthesis of14C-labelled dibenzo[d, g] [1,3,6]dioxazocine derivatives (EGYT-2474 and EGYT-2509)

Synthesis of 2-chloro-12-(3-dimethylaminopropyl)-dibenzo[d, g] [1,3,6]dioxazocine maleate (EGYT-2474) and 2-chloro-12-(3-dimethylamino-2-methylpropyl)-di-benzo[d, g] [1,3,6] dioxazocine hydrochloride (EGYT-2509) labelled with 14C-isotope is reported. The synthesis of above compounds was based on [14C] methylene diiodide which was prepared by the reduction of [14C]iodoform. [14C]Iodoform was synthesised by an improved method in a radiochemical overall yield of 44% calculated on barium [14C]carbonate.