摘要 |
<p>A process whereby both enantiomers of optically active α-hydroxy-η-butyrolactone, which are useful as medicinal intermediates, can be conveniently produced from inexpensive and easily available materials. Optically active α-hydroxy-η-butyrolactone is produced by reacting an optically active 4-amino-2-hydroxybutanoic acid derivative with nitrous acid and cyclizing under acidic conditions. Further, (S)-α-hydroxy-η-butyrolactone is reacted with sulfonyl chloride in the presence of a base to give (S)-α-sulfonyloxy-η-butyrolactone. It is further reacted with a carboxylic acid salt to give (R)-α-acyloxy-η-butyrolactone which is then deacylated by treating with an acid or a base in an alcoholic solvent to give (R)-α-hydroxy-η-butyrolactone.</p> |