NEW MATERIAL: The compd. of formula I [(n) is 1 or 2; R is H, a substituted 1-21C aliphatic group, a (substituted) 3-20C alicyclic group, a (substituted) 6-12C aliphatic group, a (substituted) 3-20C alicyclic group, a (substituted) 4-20C alicyclic-aliphatic group or the like; R2 and R3 are H, a (substituted) 1-21C aliphatic group, a (substituted) 3-20C alicyclic group, a (substituted) 6-12C aromatic group or the formula II [R4 is H, a 1-6C aliphatic group or the like), etc., where at least either R3 or R4 is the formula II].
EXAMPLE: 5-Methyl-1,3-dioxoleci-2-one-4-ylmethyl2-[N-(1S-ethoxycarbonyl-3- phenylpropyl)-S-alanyl]-(1S,3S,5S)-2-azabicyclo[3,3,0]octane-3-carboxylate.
USE: It is useful as the prodrugs of angiotensin conversion enzyme inhibitors, agents for treating hypertension, agents for treating Alzheimer's diseases or the like.
PREPARATION: A compd. of formula III is reacted with a compd. of formula IV (X is Br or the like) under the conditions of nucleophilic substitution reaction.
Urbach, Hansjoerg
Rainharuto, Betsukaa
Hock, Franz
