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An Efficient Synthesis of Risperidone via Stille Reaction: Antipsychotic, $5-HT_2$, and $Dopamine-D_2-Antagonist$  

Kim Dong-myung (PDT Bio Co. Ltd. and College of Pharmacy, Kyung Hee University)
Kang Min-Seok (PDT Bio Co. Ltd.)
Kim Jeong Sook (PDT Bio Co. Ltd.)
Jeong Jin-Hyun (PDT Bio Co. Ltd. and College of Pharmacy, Kyung Hee University)
Publication Information
Archives of Pharmacal Research / v.28, no.9, 2005 , pp. 1019-1022 More about this Journal
Abstract
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.
Keywords
Risperidone; Stille reaction; Synthesis; Antipsychotic; Dopamine-D2-antagonist;
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