Axially substitutive silicon phthalocyanine complex and doxorubicin conjugate thereof
A silicon phthalocyanine complex technology, applied in the field of axially substituted silicon phthalocyanine complexes and doxorubicin conjugates, can solve the problems of high skin phototoxicity, clinical application limitations, and unstable composition of the mixture. Achieve the effect of high cancer cell uptake rate and excellent amphiphilicity
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[0039] The preparation method of the axial terminal dipeptide substituted silicon phthalocyanine described in the formula (2.1-2.2) comprises the following steps:
[0040] 1) With the axial terminal carboxyl substituted silicon phthalocyanine and N-hydroxysuccinimide as reactants, N,N-dimethylformamide as solvent, in 1-ethyl-(3-dimethylaminopropyl In the presence of carbodiimide hydrochloride and under the protection of nitrogen, stir and react at -5~5°C for 1~2 hours, then continue to stir and react at room temperature~35°C for 12~36 hours, and then use column chromatography to separate Obtain silicon phthalocyanine carboxyl activator; Wherein, the molar ratio of axial terminal carboxyl substituted silicon phthalocyanine and N-hydroxysuccinimide is 1:1.5~5, described axial terminal carboxyl substituted silicon phthalocyanine is the axial terminal Carboxyl disubstituted silicon phthalocyanine Or axial asymmetric monocarboxy substituted silicon phthalocyanine ; The amount o...
Embodiment 1
[0054] 2-[4-(2-Aminoethyl)phenoxy]silicone phthalocyanine Synthesis
[0055] According to the published patent method (ZL201210155097.4), the specific steps are as follows:
[0056] Under nitrogen protection, dichlorophthalocyanine silicon (244.7mg, 0.4mmol), 4-(2-aminoethyl)phenol 1.2~2mmol (preferably 1.6mmol) and NaH were added to 20~50mL toluene or xylene or di Oxycycline (preferably toluene, 30mL), reflux for 12~24 hours (preferably 18 hours); vacuum rotary evaporation to remove solvent, use 100mL dichloromethane to dissolve, centrifuge to remove insoluble matter, dichloromethane solution is extracted with water (3×100mL ), collect the organic layer, then extract with dilute hydrochloric acid (0.1~0.5mmol), and collect the aqueous layer; neutralize the aqueous layer with 1M sodium hydroxide, precipitate a blue precipitate, centrifuge, wash with water, and dry in vacuo to obtain a blue product. The rate is 45%. The maximum absorption peak of the product in DMSO is loca...
Embodiment 2
[0058] Axially asymmetric monocarboxy substituted silicon phthalocyanine Synthesis
[0059] According to the published patent application (ZL201410108985.X), the specific steps are as follows:
[0060] Under the protection of nitrogen, dichlorosilicon phthalocyanine (100mg, 0.164mmol), p-hydroxyphenylpropionic acid (1.640~3.280mmol, preferably 4.920mmol) and NaH (0.01~0.02mmol, preferably 0.016mmol) were added to 7~15mL In toluene (preferably 10mL), reflux for 12-24 hours (preferably 12 hours). The solvent was removed by vacuum rotary evaporation, and washed with water to obtain a blue crude product; the crude product was dissolved in tetrahydrofuran, filtered to remove insoluble matter, and then purified by silica gel column, using ethyl acetate: tetrahydrofuran (1:1, v / v) as eluent The second fraction was collected, concentrated and dried to obtain a blue product with a yield of 35.00%. The maximum absorption peak of the product in DMF is located at 683nm, and the maximu...
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