摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new structure manifestingα,β-adrenergic antagonistic activities in an animal test, hardly causing side effect, and useful as anα/β-blocker having high activities. SOLUTION: This structure is a guaiacoxypropanolamine structure of formula I [R is CH=CHCH3 or the like; R2 is a group of formula II (R3 is OH, OCH3 or the like) or the liked, e.g. 1-[(4-allyl-2-methoxy) phenoxy]-3-[(2- methoxyphenoxyethyl)amino]-propanol. The structure of formula I is obtained by reacting an ester of formula III with ethylene bromide to provide an ester of formula IV, while reacting nonivamide with epichlorohydrin to provide an epoxide of formula V, mixing the ester of formula IV with the epoxide of formula V, and aminating the product. An excellentα,β-blocker is provided therefrom.
|