Synthesis of analogs of agrimophol

Twenty-three monomeric and dimeric acylphloroglucinol derivatives were synthesized for the purpose of finding analogs of agrimophol with higher antischistosomal activity and lower toxicity and more readily prepared as compared with agrimophol. The monomeric acylphloroglucinols were synthesized by acylating the phloroglucinol with appropriate acyl chloride or acid anhydride in the presence of borontrifluoride; the dimeric compounds were prepared by condensation of two molecules of acylphloroglucinols with formaldehyde or methoxymethylacetate. In animal screening tests compounds 1,3,14,19 and 22 exhibited antischistosomal activity.