Abstract
Synthesis of thiopurine nucleosides (and nucleotides) by the application of aminothiono exchange reaction (sulfhydrolysis) was described. 1-Methyl-6-thioinosine and 2', 3'-O-isopropylidene-5'-deoxy-3, 5'-cyclo-2-thioxanthosine were obtained from 1-methyladenosine and cycloguanosine, respectively. Sulfhydrolysis of a 3, 5'-cycloadenosine gave a 5-amino-N5, 5'-cycloimidazole-4-thiocarboxamide riboside in high yield. Synthesis of 6-thioinosine and 6-thioxanthosine by sulfhydrolysis of N6-methoxyadenosine and crotonoside, respectively, was also performed.