Applying Gewald reaction for the preparation of some novel aminothieno derivatives featuring noroxymorphone skeletal backbone

摘要

A group of noroxymorphone derivatives were subjected to Gewald reaction conditions to prepare their respective aminothieno products. In refluxing piperidine/ethanol, 1a-g reacted with elemental sulfur and malononitrile to produce 2a-g in high yields. Reactions took place in one pot and completed within 4-7 h and products precipitated spontaneously in the reaction mixtures.