Studies on the Directed Fischer Indole Synthesis

Abstract

Unnecessary carbonyl reduction step in Heathcock’s method was removed by using Cu(I)-catalyzed coupling reaction and the scope of the method was expanded : using 2-halophenol in forming N-O tether, hydrazide and various ketone compounds in Fischer indole synthesis. Ary hydrazide containing N-O tether was able to suppress the abnormal Fischer indole synthesis.