Polyethylene glycol monomethyl ether statin compound and preparation method thereof
A technology of polyethylene glycol monomethyl ether and polyethylene glycol methyl ether, which is applied in the field of polyethylene glycol monomethyl ether statins and their preparation, can solve the problems of not causing problems for Chinese people, and achieve the reduction of medicinal dosage, Low toxicity and side effects, and the effect of improving the drug loading rate
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Embodiment 1
[0025] Example 1: mPEG 3 -(Glu) 1 -(Simvastatin) 2
[0026] (1) Dissolve 0.1 mol of triethylene glycol monomethyl ether in 200 ml of tetrahydrofuran, add 3 mmol of sodium block and stir at room temperature for 30 min for 1 h, then dropwise add 0.09 mol of tert-butyl acrylate, and stir for 12 h. Quenched with water, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried. The crude product was dissolved in 200ml of dichloromethane, then 40ml of trifluoroacetic acid was added, and stirred at room temperature for 5h. After the reaction was completed, 100ml of water was added, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried to obtain a crude product. The crude product was purified by a silica gel column to obtain 0.085 mol triethylene glycol monomethyl ether propionic acid. Yield: 85%. NMR data are as follows: 1HNMR (400MHz, CDCl 3 ): δ: 3.78(t, J=4.4Hz, 2H); 3.661~3.642(m, 10H); 3.580(t, J=4.0Hz, 2H); 3.381(s,...
Embodiment 2
[0029] Example 2: mPEG 12 -(Glu) 1 -(Simvastatin) 2
[0030] (1) Dissolve 0.1 mol of dodecaethylene glycol monomethyl ether in 200 ml of tetrahydrofuran, add 3 mmol of sodium block and stir at room temperature for 1 h, then dropwise add 0.09 mol of tert-butyl acrylate, and stir for 12 h. Quenched with water, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried. The crude product was dissolved in 200ml of dichloromethane, then 40ml of trifluoroacetic acid was added, and stirred at room temperature for 5h. After the reaction was completed, 100ml of water was added, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried to obtain a crude product. The crude product was purified by a silica gel column to obtain 0.088 mol of dodecaethylene glycol monomethyl ether propionic acid. Yield: 88%. NMR data are as follows: 1HNMR (400MHz, CDCl 3 ): δ: 3.97(t, J=4.4Hz, 2H); 3.668~3.6420(m, 46H); 3.586(t, J=4.0Hz, 2H); 3.378(s,...
Embodiment 3
[0033] Example 3: mPEG 24 -(Glu) 1 -(Simvastatin) 2
[0034] (1) Dissolve 0.1 mol of tetracosane glycol monomethyl ether in 200 ml of tetrahydrofuran, add 3 mmol of sodium block and stir at room temperature for 30 min, then dropwise add 0.09 mol of tert-butyl acrylate, and stir for 12 h. Quenched with water, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried. The crude product was dissolved in 200ml of dichloromethane, then 40ml of trifluoroacetic acid was added, and stirred at room temperature for 5h. After the reaction was completed, 100ml of water was added, extracted with dichloromethane, dried over anhydrous sodium sulfate, and spin-dried to obtain a crude product. The crude product was purified by a silica gel column to obtain 0.09 mol tetracethylene glycol monomethyl ether propionic acid. Yield: 90%. NMR data are as follows: 1HNMR (400MHz, CDCl 3 ): δ: 3.76(t, J=4.4Hz, 2H); 3.651~3.632(m, 94H); 3.580(t, J=4.0Hz, 2H); 3.378(s, 3H);...
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