Enantioselective enzymatic acylation of 1-(3′-bromophenyl)ethylamine |
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| Institution: | 1. Process Research and Development, Bristol-Myers Squibb Pharmaceutical Research Institute, New Brunswick, NJ, USA;2. Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Lawrenceville, NJ, USA |
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| Abstract: | An efficient biocatalytic process has been developed for the resolution of 1-(3′-bromophenyl)ethylamine (RS)-1 by way of enantioselective lipase-mediated (R)-selective acylation with ethyl 2-methoxyacetate to afford (S)-amine (S)-1 and (R)-2″-methoxyacetamide ((R)-2) in 91–95% and 90–92% isolated yield, respectively, and both with >99% ee. |
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