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Synthetic studies on psychotropic agents part 1 a new synthesis of 2 amino 4 fluoro butyrophenone derivatives using a selective ortho amination of 2 4 di fluoro butyrophenone derivatives



Synthetic studies on psychotropic agents part 1 a new synthesis of 2 amino 4 fluoro butyrophenone derivatives using a selective ortho amination of 2 4 di fluoro butyrophenone derivatives



Chemical and Pharmaceutical Bulletin 26(8): 2502-2507



A new synthesis of the potent neuroleptic 2'-amino-4'-fluoro-4-[4-hydroxy-4-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)piperidino]butyrophenone using a selective ortho-amination as a key step was described. The solvents and temperature effects on the selectivity for this ortho-amination of 2',4'-difluoro-4-[4-hydroxy-4-(.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)piperidino]butyrophenone were investigated.

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