Preparation method and application of polyethylene glycol monomethyl ether modified abiraterone compound
A technology of polyethylene glycol monomethyl ether and abiraterone, which is applied in the direction of steroidal compounds, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of complicated preparation process and ineffective drug effect Significantly improved, difficult to achieve large-scale production and other problems, to achieve high yield, simple preparation method, good water solubility
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Embodiment 1
[0045] Example 1 Synthesis of polyethylene glycol monomethyl ether modified abiraterone compound 2a
[0046] 1 mmol methoxy polyethylene glycol and 2mmol of succinic anhydride were dissolved in 1.0ml of toluene, 0.5mmol of triethylamine was added, the temperature was rapidly raised to 60°C, stirred for 12h, the reaction was monitored by TLC (dichloromethane:methanol=8:1), and the color was developed by iodine fumigation. After the reaction was completed, water was added, extracted with dichloromethane three times, the organic layer was washed twice with 1M HCl, and then three times with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain methoxypolyethylene glycol butyl. Diester, yield 95%. Dissolve 1 mmol of methoxy polyethylene glycol succinate, 1.2 mmol of abiraterone and 0.5 mmol of 4-dimethylaminopyridine (DMAP) in 10 ml of dichloromethane, add 1.0 mmol of dicyclohexylcarbodiimide ( DCC), the reaction was stirred at room temperature for 20h. ...
Embodiment 2
[0047] Example 2 Synthesis of polyethylene glycol monomethyl ether modified abiraterone compound 2b
[0048] 1 mmol methoxy polyethylene glycol and 2mmol of succinic anhydride were dissolved in 1.0ml of toluene, 0.5mmol of triethylamine was added, the temperature was rapidly raised to 60°C, stirred for 12h, the reaction was monitored by TLC (dichloromethane:methanol=8:1), and the color was developed by iodine fumigation. After the reaction was completed, water was added, extracted with dichloromethane three times, the organic layer was washed twice with 1M HCl, and then three times with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain methoxypolyethylene glycol butyl. Diester, yield 93%. Dissolve 1 mmol of methoxy polyethylene glycol succinate, 1.2 mmol of abiraterone and 0.5 mmol of 4-dimethylaminopyridine (DMAP) in 10 ml of dichloromethane, add 1.0 mmol of dicyclohexylcarbodiimide ( DCC), the reaction was stirred at room temperature for 20h. ...
Embodiment 3
[0049] Example 3 Synthesis of polyethylene glycol monomethyl ether modified abiraterone compound 2c
[0050] 1 mmol methoxy polyethylene glycol and 2mmol of succinic anhydride were dissolved in 1.0ml of toluene, 0.5mmol of triethylamine was added, the temperature was rapidly raised to 60°C, stirred for 12h, the reaction was monitored by TLC (dichloromethane:methanol=8:1), and the color was developed by iodine fumigation. After the reaction was completed, water was added, extracted with dichloromethane three times, the organic layer was washed twice with 1M HCl, and then three times with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain methoxypolyethylene glycol butyl. Diester, yield 91%. Dissolve 1 mmol of methoxy polyethylene glycol succinate, 1.2 mmol of abiraterone and 0.5 mmol of 4-dimethylaminopyridine (DMAP) in 10 ml of dichloromethane, add 1.0 mmol of dicyclohexylcarbodiimide ( DCC), the reaction was stirred at room temperature for 20h. ...
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