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[求助]
大神们,显神通!求翻译一段英文,有BB感谢!
In order to establish whether the overall reaction from enan-tiomer pure N -Boc-phenylalanine leads to any loss of optical purity through partial racemization in presence of base, enantiomeric excess (ee) values of L-Ia and diastereoisomeric excess (de) values based on the stereoconfi guration of amino acid amide part of fi nal product L -IIa obtained from L -N-Boc-phenylalanine were deter-mined. While Boc-deprotected product (free amine) showed an ee of 99.4%, the target compound L-IIa arising through nucleophilic addition of L- Ia on a-phosphateisothiocyanate was obtained in 98.5% de. Thus, as expected, stereochemical configuration at a-carbon atom of the acid was practically unaffected and this synthetic transformation from chiral a-amino acid could be applied to a wide range of compounds without undergoing any signi fi cant loss of optical activity. Since both L- and D -isomers of N -Boc- phenylalanine are easily accessible, it provides a useful route to obtain both the enantiomeric forms of carboxamideIa e c which are useful synthons to a variety of pharmaceuticals. The overall process for novel (L)/(D)- pseudo-peptide thioureasIIae l is convenient, high yielding and atom-economic.
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