abstract |
PURPOSE: To provide new amino acid derivatives which are effectively used as a synthetic intermediate for a derivative of cis, endo-azabicyclo [3,3,0]- octane-carboxylic acid having blood pressure reduction activity of long persistence. n CONSTITUTION: This amino acid derivative id represented by formula I [R 1 is allyl, vinyl, a side chain of naturally occurring α-aminoacid, R 1 -CH(NH 2 ) -COOH; R 2 ' is 1-6C alkyl, 2-6C alkenyl, aryl 1-4C alkyl; X is 1-6C alkyl, 2-6C alkenyl, 5-9C cycloalkyl, 6-12C aryl, indol-3-yl; W' is a group which is decomposable by hydrogenation, base or acid, R 2 ' is not benzyl or nitrobenzyl when W' is benzyl], e.g. N-(1-S-carboethoxy-3-phenyl-propyl)-S-alanyl-2-cis,endo- azabicyclo[3,3,0] octane-3-S-carboxylic acid. The compound of formula I is produced from a compound of formula II (X is aryl). n COPYRIGHT: (C)1992,JPO |