Synthesis of 2‐amino‐3,5‐dihydro‐7‐(3‐thienylmethyl)‐[6‐14C]‐4H‐pyrrolo[3,2‐d]pyrimidin‐4‐one monohydrochloride ([14C]CI‐1000)

Abstract

Abstract2‐Amino‐3,5‐dihydro‐7‐(3‐thienylmethyl)‐[6‐14C]‐4H‐pyrrolo [3,2‐d]pyrimidin‐4‐one monohydrochloride ([14C]Cl‐1000), a potent purine nucleoside phosphorylase inhibitor, was made in six steps from potassium [14C]cyanide. A key step was the reduction of a nitro and a nitrile group with sodium hypophosphite and RaNi followed by cyclization of the resulting intermediate to form a pyrrolo[3,2‐d] pyrimidinone.