Effects of nitrogen and alkene substitution on the PtCl2 catalyzed cycloisomerization of N-tethered 1,6-enyne precursors to the triple reuptake inhibitor GSK1360707 |
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| Authors: | Vassil Elitzin Bing LiuMatthew Sharp Elie Tabet |
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| Affiliation: | Product Development, API Chemistry and Analysis, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA |
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| Abstract: | The effects of nitrogen and alkene substitution on the cycloisomerization of N-tethered 1,6-enynes into 3-azabicyclo[4.1.0]heptene precursors to the triple reuptake inhibitor GSK1360707 are described. In general, electron donating substituents proved beneficial both in terms of the reaction rate and chemoselectivity. |
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| Keywords: | 1,6-Enyne cycloisomerization Pt(II) catalysis Au(I) catalysis Nitrogen substitution effect Alkene substitution effect |
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