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酞菁类化合物(图1)在长波区(600-700nm)有强吸收,制备简单,稳定性好,可能成为取代血卟啉的新一代光动力药物.在实际使用时,要求酞菁具有一定程度的水溶性,这就需要在酞菁环上引入亲水基团.利用缩合法和直接磺化法,可以在酞菁的四个苯环上引入磺酸基团,前者只在苯环的4位上连有磺酸基,而后者得到的是3,4位磺酸取代的混合物,平均磺化程度取决于反应条件.动物实验表明,由于二聚程度和对细胞组织穿透能力不同,磺化度对光疗效果影响很大.因此必须探索合适的合成条件和磺化度分析方法.直接磺化得到的往往是几种甚至十几种组分的混合物,而且分离除去共生的无机盐比较困难,用一般的分析磺化度的方法难以得到准确的结果.由于不同组分的磺化酞菁用浓硝酸氧化
Phthalocyanines (Figure 1) have strong absorption in the long-wave region (600-700nm), and are simple to prepare and have good stability, which may become a new generation of photodynamic drugs instead of hematoporphyrin. In actual use, phthalocyanines are required The degree of water-soluble, which requires the introduction of hydrophilic groups on the phthalocyanine ring.Using the condensation method and direct sulfonation method, the phthalocyanine can be introduced on the four benzene ring sulfonic acid group, the former only in the benzene ring Sulfonic acid group is attached to the 4 position, while the latter is a 3,4-sulfonic acid substituted mixture, the average degree of sulfonation depends on the reaction conditions.Experimental results show that due to the degree of dimerization and the ability to penetrate different cell tissues, Sulfonation degree has a great influence on the phototherapy effect, so it is necessary to explore the appropriate synthesis conditions and sulfonation degree analysis methods.Direct sulfonation obtained often is a mixture of several or even a dozen components, and the separation and removal of symbiotic inorganic salts Difficult to use the general method of analysis of the degree of sulfonation difficult to get accurate results due to the different components of sulfonated phthalocyanine with concentrated nitric acid oxidation