Porretta G C, Filacchioni G, Stefancich G, Giuliano R, Artico M
Farmaco Sci. 1978 Apr;33(4):263-70.
Intramolecular cyclization of 1-(2-carboxy-4-nitrophenyl)pyrrole afforded 7-nitro-9-oxo-9H-pyrrolo[1,2-a]indole, which was then reduced to 7-amino-9-oxo-9H-pyrrolo[1,2-a]indole. The same procedure was adopted for the synthesis of 6-amino-9-oxo-9H-pyrrolo[1,2-a]indole starting from 1-(2-carboxy-5-nitrophenyl)pyrrole. The preparation of some N-acylderivatives of the above cited aminoketones is reported. These compounds shall be subjected to biological screening against Leukemia L 1210 as a simple analogues of Mitomycin C.
1-(2-羧基-4-硝基苯基)吡咯的分子内环化反应生成了7-硝基-9-氧代-9H-吡咯并[1,2-a]吲哚,随后将其还原为7-氨基-9-氧代-9H-吡咯并[1,2-a]吲哚。从1-(2-羧基-5-硝基苯基)吡咯开始合成6-氨基-9-氧代-9H-吡咯并[1,2-a]吲哚采用了相同的步骤。报道了上述氨基酮的一些N-酰基衍生物的制备。这些化合物将作为丝裂霉素C的简单类似物针对白血病L 1210进行生物筛选。