Novel cationic polymer used for non-virus type gene carrier, its preparation method and its purpose
A kind of cationic polymer and polymer technology, which is applied in the direction of introducing foreign genetic material, gene therapy, and pharmaceutical formulations by using carriers, and can solve problems such as in vivo application limitations, degradation, and cytotoxicity
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Embodiment 1
[0060] Embodiment 1 contains the synthesis of the alkynylated diethylenetriamine monomer (numbering A) of Boc
[0061] Diethylenetriamine (1.03g, 10mmol) was dissolved in dichloromethane DCM (50mL). After cooling in an ice bath, ethyl trifluoroacetate (2.95g, 21mmol) was added dropwise, and stirred in an ice bath for 1h. After the temperature of the reaction solution rose to room temperature and then stirred for 1 h, di-tert-butyl dicarbonate Boc dissolved in an appropriate amount of DCM was added dropwise. 2 O (3.28g, 15mmol) solution and triethylamine TEA (1.52g, 15mmol) solution were stirred at room temperature overnight. with saturated NaHCO 3 Washed with saturated brine, anhydrous Na 2 SO 4 dry. After concentration, it was recrystallized with DCM / n-hexane system. The recrystallized material (2.00g) contained K 2 CO 3 (1.80 g) was refluxed in methanol / water (volume ratio 20:1) system for 4 h, methanol was spin-dried, and the residue was extracted with DCM (3×100 mL)...
Embodiment 2
[0063] Embodiment 2 contains the synthesis of the alkynylated triethylenetetramine monomer (numbering B) of Boc
[0064] Triethylenetetramine (1.46g, 10mmol) was dissolved in DCM (50mL) solution, and after cooling in an ice bath, ethyl trifluoroacetate (2.95g, 21mmol) was added dropwise, and stirred in an ice bath for 1h. After the temperature of the reaction solution rose to room temperature and then stirred for 1 h, Boc dissolved in an appropriate amount of DCM was added dropwise. 2 O (5.68g, 26mmol) solution and TEA (2.63g, 26mmol) solution were stirred at room temperature overnight. with saturated NaHCO 3 Washed with saturated brine, anhydrous Na 2 SO 4 dry. After concentration, it was recrystallized with DCM / n-hexane system. The recrystallized material (2.00g) contained K 2 CO 3 (1.80 g) was refluxed in methanol / water (volume ratio 20:1) system for 4 h, methanol was spin-dried, and the residue was extracted with DCM (3×100 mL). The combined organic phases were was...
Embodiment 3
[0066] Synthesis of embodiment 3 azide diethylene glycol monomer (numbering 1)
[0067] Diethylene glycol (2.12 g, 20 mmol) was dissolved in DCM (250 mL) and cooled in an ice bath. Add p-toluenesulfonyl chloride (7.62g, 42mmol), TEA (4.25g, 42mmol) and 4-dimethylaminopyridine DMAP (0.12g, 0.1mmol) in sequence, stir in ice bath for 1h, and then stir at room temperature for 12h. The reaction solution was sequentially washed with saturated NaHCO 3 (2×300mL) and saturated brine (300mL) for washing, anhydrous Na 2 SO 4dry. After concentration, it was recrystallized with DCM / n-hexane system. Dissolve the recrystallized product (4.1 g, 10 mmol) in acetone, add sodium azide (1.9 g, 30 mmol), and reflux for 48 h. The solvent was concentrated, separated by silica gel column chromatography, and eluted with petroleum ether / ethyl acetate (volume ratio 2:1) to obtain monomer 1 ( 1 HNMR (DMSO-d 6 ): 2.87(s, 4H), 2.70(s, 4H)). The structural formula of monomer 1 is as follows:
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