Studies toward the total synthesis of the variolins:rapid entry to the core structure

摘要

The pyrido[3',2',4,5]pyrrolo[1,2-c]pyrimidine core structure of the variolins has been synthesized in three steps from commercially available materials.The key reaction involves the deoxygenation and concomitant cyclization of a triarylmethanol using the combination of triethylsilane and trifluoroacetic acid.Introduction of amine functionality as required for the natural products has been achieved in two steps.