An efficient method for the synthesis of tri-substituted 1,3,5-triazine derivatives based on Ru-catalyzed reaction of alcohols with biguanides is presented.

An efficient ruthenium-catalyzed synthesis of alkyl-1,3,5-triazies from arylallyl alcohols and biguanides has been developed. The reaction occurred in moderate to good yields and tolerated heterocyclic or aryl allyl alcohols containing functionalities such as alkanes, ethers, and halogens. The reaction proceeds through a one-pot sequence of transfer hydrogenation and condensation steps.

During the course of studies on the production and isolation of macrocyclic trichothecenes from fungal isolates,l) we have developed procedures