Condensation of 6-chloro-2-iodo-9-isopropylpurine (I) with 4-chlorobenzylamine (II) in hot EtOH afforded the 6-(benzylamino)purine (III). Subsequent Suzuki coupling of (III) with 3-methylpent-1-yn-3-ol (IV) in the presence of Pd(0) and CuI produced the target 2-ethynylpurine derivative.