PURPOSE: To obtain a new propenone derivative having excellent antitumor activity.
CONSTITUTION: This compound is shown by formula I [R1 is H or a lower alkyl or a (substituted) bicyclic aromatic ring of formula II or formula III (R2 to R4 are each H, an aroyl, etc.; Y1 and Y2 are each H or Y1 and Y2 are bonded to form O; (a) is NH or O)] or its salt such as (E)-3-(naphthalene-2-yl)-1-(3,4,5- trimethoxyphenyl)-2-propene-1-one. The compound is obtained by reacting a compound of formula IV such as 3',4',5'-trimethoxyacetophenone, etc., with a compound of formula V such as naphthalene-2-carboxyaldehyde, etc., in the presence of a base such as piperidine, etc., in an inert solvent such as methanol at -78°C to the boiling point of the solvent for 0.1 hour to seven days. The compound of formula V, for example, is obtained from 3,4,5- trimethoxybenzaldehyde as a starting substance.
KIMURA UICHIRO
ASHIZAWA TADASHI
GOMI KATSUNARI
SAITO HIROMITSU