Chapter 1 Benzoheteropines with Fused Pyrrole, Furan and Thiophene Rings

Abstract

Publisher Summary Heteropines received much attention, primarily because of continuous interest in the psychopharmacological activity of their bicyclic and tricyclic derivatives. Synthesis, structures, reactivity, and applications of tricyclic heteropines have been a part of the general indole and seven-membered rings discussions. It surveyed the synthesis of 1,5-benzodiazepines with three-, four- and five-membered rings fused to different positions of the 1,5-benzodiazepine skeleton. The synthesis of DNA-interactive pyrrole[ 2, l-c][1,4] benzodiazepines and medicinal chemistry aspects of the novel thieno benzodiazepine antipsychotic, Olanzapine, have been reviewed. This chapter focuses on the benzoheteropines with the fused pyrrole, thiophene, or furan rings that is ortho-fused 6+7+5 ring systems with carbons only on the six-membered ring, one heteroatom on the five-membered ring and one or more heteroatoms on the seven- membered ring. The variety of heteroatoms is limited to nitrogen, oxygen, and sulfur. Several examples of the related cyclic systems with the other heteroatom distribution or peri-fusion are briefly summarized in the chapter.