抄録
The reaction of 2-amino-1, 5-benzodiazocine 1-oxides (1) with acetylenecarboxylates (2, 11) afforded C(10)-alkylated derivatives (3) via 3, 3-sigmatropic rearrangement. Compounds 3 gave 10-alkoxycarbonylmethyl-1, 5-benzodiazocines (4) when heated in ethanol. Heating of 3a-e in pyridine, on the other hand, gave indole derivatives (9), which were converted into 7-benzoylindoles (10a-e) by acid hydrolysis. The reaction of 2-amino-1, 4-benzodiazepine 1-oxides (13) with acetylenedicarboxylates (11) also gave the rearranged products (14).
