| 摘要 |
PURPOSE:To obtain the titled compound useful as a synthetic intermediate for a certain physiologically active substance in high purity and in high yield by an easy process, by treating a succinic acid derivative or its antipode with a tertiary amine. CONSTITUTION:A compound shown by the formula I (R is substitutent group commonly used for the protection of functional group; X is halogen), its antipode is treated with a tertiary amine, preferably triethylamine, to give the titled compound shown by the formula II or its antipode. Especially, the reaction product is only allowed to stand at room temperature for 24hr to give the compound shown by the formula II almost quantitatively. (2S, 3S)-Epoxysuccinate among the compound shown by the formula II is an important synthetic intermediate for N-[N- (L-3-trans-carboxyoxysilane-2-carbonyl)-L-leucyl]agmatine inhibiting an enzyme (CANP) showing extraordinary high activity in the muscle of the affect part of a muscular dystrophy patient. |
