METHOD FOR THE PRODUCTION OF ANTHELMINTHICALLY EFFECTIVE BASIC SUBSTITUTED 2-CARBALKOXYAMINO-BENZIMIDAZOLYL-4 (6)-PHENYLATHERS UN-KETONES

摘要

Basic substd. 2-carbalkoxyamino-benzimidazolyl-5(6)-phenylethers and -ketones are of formula (I): (where R3 is 1-4C alkyl, X -O, -S or C=O, Y=opt. branched 1-4C alkylene; R1 and R2 is 1-4C alkyl or R1R2N may form a pyrrolidine-, piperidine, morpholine, or thiomorpholine ring. They are prepd. by reacting cpds of formula (II) (as I, COOR3 replaced by H) with O=C(OR3)-(OR4) in the presence of a strong base (where R3 and R4 are independently 1-4C alkyl, phenyl, or p-nitrophenyl. The starting 2-aminobenzimidazole derivs. (II) are also disclosed as novel. (I) have anthelmintic activity and may be used as chemotherapeutics against parasitic diseases in human and veterinary medicine. They are esp. active against ankylostomae as well as against other helminths. (I) are very active against hookworm in man, carnivores and ruminants. Dosage 0.5-50 mg/kg for 1-4 days.