PYRROLIDINE DERIVATIVE

摘要

NEW MATERIAL:The compound of formula I [X is H, halogen or lower alkyl; R is (substituted) alkyl, (substituted) naphthyl or heteroaryl] or its salt. EXAMPLE:(+ or -)-trans-3-(2-Chloro-3-hydroxyphenyl)-4-(3,4-dihydroxyphenyl)pyrrolidine hydrobromide. USE:A drug. A remedy and preventive for diseases to which dopamine 1 agonist action is effective. A remedy and preventive for hypertension or remedy and preventive for cardiac insufficiency. PREPARATION:The trans-isomer of the compound of formula I can be produced by adding a compound of formula IV (R<6> is OH-protecting group; R<7> is lower alkyl) to a compound of formula V to produce a compound of formula VI as an addition reaction product, reducing the compound to a compound of formula VII, cyclizing the product to obtain a compound of formula VIII, isomerizing to a transisomer, reducing the isomer and finally removing the protecting groups.