An efficient synthesis of risperidonevia stille reaction: Antipsychotic, 5-HT2, and dopamine-D2-antagonist

• DOI: 10.1007/bf02977394
• Publication Date: 2008-11-26T13:48:11Z
• Authors: Dong-myung Kim; Min-Seok Kang; Jeong Sook Kim; Jin-Hyun Jeong
• Keywords: Dopamine D2 Receptor Antagonists; Serotonin 5-HT2 Receptor Antagonists; Dopamine Antagonists; Serotonin Antagonists; Risperidone; 01 natural sciences; Antipsychotic Agents; 0104 chemical sciences; 3. Good health

Risperidone has been reported to have neuroleptic activity. In this study, risperidone was synthesized using a new method involving a stille reaction, in which 2-methyl-3-vinyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one was synthesized (5). The chemical synthesis process was found to be simple and produced risperidone in a high yield. In addition, can be easily scaled up for large scale synthesis.