BENZOFURAN DERIVATIVE AND ITS PREPARATION

NEW MATERIAL:The compound of formula I (R1 is halogen; R2 is halogen or OH; R3 is lower alkanoyl, benzoyl, lower alkyl, benzyl or group of formula II; n is 2 or 3; the substituted aminopropoxy group is substituted to an arbitrary position in 4, 5, 6 and 7 positions of the benzofuran ring) and its acid addition salt. EXAMPLE:2-Acetyl-7-[3-[di(2-chloroethyl)amino]-2-hydroxypropoxy]-benzo furan. USE:It has antineoplastic activity, and is useful for the prevention and remedy of cancer. PREPARATION:The compound of formula I can be produced by halogenating the benzofuran derivative of formula III (R4 is lower alkanoyl, etc.) with a halogenation agent such as thionyl chloride. The reaction may be carried out in a proper solvent such as benzene. A desirable result can be attained by reacting at 10 deg.C- refluxing temperature for 30min-3hr.