pepuchida - ze inhibition active chemical compound and its manufacturing method and application

摘要

NEW MATERIAL:The compound of formula I (R is -CH3 or group of formula II or III). EXAMPLE:N-(4-phenyl-n-butanoyl)-alanyl-Pro-ol (Pro-ol is group of formula IV). USE:Medical drug. A prolylendopeptidase-inhibiting agent and antiamnestic agent. PREPARATION:The compound of formula I can be produced by dissolving the ester of formula V (R' is CH3 of lower alkyl) and NaBH4 in tert-butyl alcohol, reacting with methanol under refluxing to produce the alcohol of formula VI and oxidizing the alcohol with sulfur trioxide-pyridine complex in dimethyl sulfoxide.