Fused pyrido azepines

Classical methodology was used to prepare the dibenz[b,f]azepine derivative 21 (R = substituted pyrido[2,3-d]pyrimidine) utilising amide ion formation from dibenz[b,f]azepine itself with sodium hydride and then iV-alkylation with 2,4-diamino-6-bromomethylpyrido[2,3-d]pyrimidine. The bulky bis-fused azepine moiety was required to introduce steric bulk in the system and to study the effect of this on inhibition of the enzyme dihydrofolate reductase <00JHC921>. 

This review is based on Mosby s book cited above and covers the literature through 2009 together with several articles published in 2010. It includes pyrido[l,2-fl]azepines and their hydro products as well as linearly or angularly fused benzo and dibenzo derivatives. Patents are taken into account provided they reveal important aspects of synthesis or application. 

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