抗抑郁药帕罗西汀去氟杂质的合成

Synthesis of the Defluorinated Impurity of Antidepressant Paroxetine Hydrochloride

(3S,4R)-4-苯基-3-{[(3,4-亚甲氧基)苯氧基]甲基}哌啶是抗抑郁药盐酸帕罗西汀合成中的一个副产物,对研究盐酸帕罗西汀成品的质量具有较大价值。本文以(3S,4R)-4-(4-氟苯基)-3-羟甲基-1-甲基哌啶为起始原料,依次经脱氟、酯化、醚化、脱甲基成盐、碱化游离后得到纯度在99%以上的去氟帕罗西汀,合计收率约39.5%。

（3S,4R）-4-phenyl-3-[[（3,4-methylenedioxy）phenoxy]methyl]piperidine was a by-product when producing the antidepressant paroxetine. It has a great value to studying the quality of paroxetine. In order to synthesize it, （3S, 4R）-4-（4-Fluorophenyl）-3-hydroxymethyl-l-methylpiperidine used as the starting material, vial defluorination, esterification, etberification, demethyllation and saltification, and alkalization, get the purity of the product more than 99 %. The total yield of this synthetic route can get to 39.5 %.