| 摘要 |
NEW MATERIAL:A compound of the formula (R is H or lower alkyl such as methyl or ethyl, etc.) and a salt and hydrate thereof. EXAMPLE:4-Amino-3-hydroxy-6-methylheptanoyl-alanine. USE:Useful as an intermediate raw material for pepstatin derivatives, useful as a remedy for ascitic retension caused by peptic ulcer, arthritis, renal hypertension and malignant tumor, etc. PREPARATION:Pepstatin is dissolved or suspended in an acid, e.g. hydrochloric acid or sulfuric acid, and hydrolyzed at room temperature or under heating to give the compound of the formula. Preferably, the hydrolysis is carried out in concentrated hydrochloric acid at room temperature for 3-12 days. In the process, a lower alkanol, e.g. methanol, is added to the reaction mixture to afford a methyl ester derivative thereof [a compound of the formula (R is methyl)].
|
