Efficient Heck arylations of cyclic and acyclic acrylate derivatives using arenediazonium tetrafluoroborates. A new synthesis of the antidepressant drug (+/-)-paroxetine |
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Authors: | Pastre Julio Cezar Duarte Correia Carlos Roque |
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Institution: | Instituto de Química, Universidade Estadual de Campinas, UNICAMP, C.P. 6154, 13083-970, Campinas, S?o Paulo, Brazil. |
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Abstract: | reaction: see text] The Heck arylation of acyclic- and cyclic-substituted acrylates using several arenediazonium tetrafluoroborates was investigated. Arylations were carried out under aerobic, ligand-free conditions to provide the corresponding substituted acrylates in moderate to high isolated yields. Heck arylations were usually completed in less than 2 h in refluxing methanol. The aza-endocyclic acrylate derivative 11a was converted into the antidepressant drug (+/-)-paroxetine in a concise new route in good overall yield. |
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