| 摘要 |
PURPOSE:To readily obtain a compound useful for a synthetic intermediate of carbapenem based beta-lactam antibiotics or penem based beta-lactam antibiotics in high yield, by de-silylation of betalactam compound with mineral acid or organic strong acid. CONSTITUTION:A compound expressed by formula I is reacted with a mineral acid or an organic strong acid in an organic solvent or a hydrated organic solvent (e.g., acetonitrile or hydrated acetonitrile) at -20 deg.C-room temperature. Next, resultant compound is neutralized, dehydrated as necessary, filtrated, condensed and recrystallized to afford the aimed substance expressed by formula II. 0.3-10mol equiv. mineral acid or organic strong acid is used to the compound expressed by formula I. Hydrofluoric acid, hydrochloric acid, hydrobromic acid or sulfuric acid as mineral acid, or trifluoroacetic acid, paratoluenesulfonic acid or trichloroacetic acid as organic strong acid is used. |
