硝基四苯基卟啉及其衍生物的合成

Synthesis of Meso-(p-nitrophenyl)-porphyrin and Its Derivatives

质量分数65%的浓硝酸与硝基四苯基卟啉(TPP)反应较完全且没有副产物生成,单硝化TPP(m-NTPP)的收率达到约80%;其他试剂由于活性太高,生成较多的副产物而收率不高.结果表明,氮氧化合物气体在TPP硝化反应中起到关键作用.具有生物活性的小分子与还原m-NTPP所得的单氨基TPP(m-ATPP)连接,得到收率大于90%的氨基TPP衍生物,它们具有较氨基TPP更高的光动力疗法(PDT)抗肿瘤活性,同时对正常细胞的毒性降低.

The yield of mono nitro TPP reaches 80% through the reaction of 65% concentrated nitric acid and TPP,and little byproduct is found. However,the yields are low with other reagents due to much byproduct from their too high activity. Compounds are attached to amino TPP from reduction of nitro TPP in over 90% yields, PDT activity of which is improved accompanying with reduced toxicity.