Ligand-free palladium catalysed Heck reaction of methyl 2-acetamido acrylate and aryl bromides as key step in the synthesis of enantiopure substituted phenylalanines |
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| Authors: | Charlotte E Willans |
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| Affiliation: | DSM Pharma Chemicals, Advanced Synthesis, Catalysis & Development, P.O. Box 18, 6160 MD Geleen, Netherlands |
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| Abstract: | A range of substituted aryl bromides were coupled with methyl 2-acetamido acrylate using ligand-free palladium catalysis. Subsequently asymmetric hydrogenation with Rh/MonoPhos yielded substituted phenylalanines in high enantioselectivities (e.e. 92-99%). |
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| Keywords: | Ligand-free Palladium Heck Substituted phenylalanines MonoPhos |
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