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KMID : 0369919970120000019
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Journal of Pharmaceutical Sciences (C.B.N.)
1997 Volume.12 No. 0 p.19 ~ p.32
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Chemical Transfornation of Amino acid(I)
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Abstract
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2-Aminobutanol which is one of 2-amino alcohol reductive form of a-amino acid, is used as a precursor of (+)-EthambutoI. 2-Aminobutanol used in synthesis of (+)-ethambutol, is (S) (+) 2-aminobutauol produced by resolution of recemic 2-aminobutanol. But (R) (-) 2-aminobutanol produced with (S) (+) 2-aminobutanol in resolution is useless, so this synthetic method is disadvantageous. We developed inversion method of 2-aminobutanol that is SN₂ reaction as a key step that N.N-ditosylimides derivatives of
2-aminobutanol with NaN₃ in DMF at 100℃. (R) (-) 2-aminobutanol which is now abandoned can be inverted to (S) (+) 2-aminobutanol available to (+) etbainbutol by this method.
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KEYWORD
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