Polyglutamic acids functionalized by cationic groups and hydrophobic groups and applications thereof, in particular therapeutic applications thereof
A technology of cationic group and hydrophobic group, applied in the field of new biodegradable materials, can solve the problems of undocumented polyglutamate skeleton, etc., and achieve the effect of good combination
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Embodiment 1
[0197] Example 1: Synthesis of Polymer (1)
[0198]
[0199] Symbols and groups: T=D, L-α-tocopherol, p=s=11, q=198
[0200] 10 g of poly(glutamic acid) with a degree of polymerization (DP) of 220 optionally incorporated with 5% of racemic α-tocopherol was dissolved in 125 ml of NMP at 80°C. The solution was cooled to 0°C, and 8.7 ml of isobutyl chloroformate and 7.35 ml of N-methylmorpholine were added. The reaction mixture was stirred at 0 °C for 15 min. At the same time, 24.67 g of arginine amide dihydrochloride was suspended in 308 ml of NMP, and 14.7 ml of triethylamine was added. The resulting suspension was stirred at 20°C for several minutes and then cooled to 0°C. Then, a milky suspension of activated polymer was added to this suspension and the reaction mixture was stirred at 0 °C for 2 h and then at 20 °C overnight. 2.1 ml of 35% HCl solution was added, followed by 100 ml of water. The reaction mixture was dropped dropwise into 1.6 l of water. The solution ...
Embodiment 2
[0201] Example 2: Synthesis of polymers (2)
[0202]
[0203] Symbols and groups: T=D, L-α-tocopherol, p=s=6, q=108
[0204] 3.5 g of poly(glutamic acid) with a degree of polymerization (DP) of 120 optionally incorporated with 5% of racemic α-tocopherol was dissolved in 70 ml of NMP at 80°C. The solution was cooled to 0° C., and 3.2 g of isobutyl chloroformate and 2.37 g of N-methylmorpholine were added. The reaction mixture was stirred at 0 °C for 10 min. Meanwhile, 4.62 g of N-tert-butyloxycarbonyl-1,4-butanediamine (BOC-putrescine) was dissolved in 9 ml of NMP, followed by cooling to 0°C. A milky suspension of activated polymer was then added to this solution and the reaction mixture was stirred at 0 °C for 2 h and then at 20 °C overnight. After adding 0.7 ml of 35% HCl solution, the reaction mixture was dropped dropwise into 317 ml of water. The resulting solution was adjusted to pH = 7.4 with 1N sodium hydroxide solution, then dialyzed against aqueous saline soluti...
Embodiment 3
[0205] Example 3: Synthesis of polymers (3)
[0206]
[0207] Symbols and groups: T=D, L-α-tocopherol, p=11, q=88, r=99, s=22
[0208] 10 g of poly(glutamic acid) with a degree of polymerization (DP) of 220, optionally conjugated with 5% of racemic α-tocopherol, was dissolved in 125 ml of NMP at 80°C. The solution was cooled to 0°C, and 9.1 ml of isobutyl chloroformate and 7.71 ml of N-methylmorpholine were added. The reaction mixture was stirred at 0 °C for 15 min. At the same time, 8.2 g of arginine amide dihydrochloride was suspended in 103 ml of NMP, and 9.31 ml of triethylamine was added. A further 1.6 ml of ethanolamine were added and the resulting suspension was stirred at 20°C for several minutes and then cooled to 0°C. Then, a milky suspension of activated polymer was added to this suspension and the reaction mixture was stirred at 0 °C for 2 h. 1.2 ml of ethanolamine were added, followed by stirring overnight at 20°C. 2.1 ml of 35% HCl solution and 200 ml of ...
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