Amphipathic phospholipid molecule with reducing response and application thereof in drug sustained release
An amphiphilic phospholipid, responsive technology, which can be used in medical preparations with non-active ingredients, phosphorus-organic compounds, organic chemistry, etc., and can solve the problems of limited use of reducing agents, difficulty in separation and purification, and cumbersome synthesis of reduction-responsive vesicles.
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[0034]
[0035] Synthetic route: a. 2,2'-dithiodipyridine, triethylamine, 0°C; b. Mercaptopropionic acid, triethylamine, dichloromethane, 25°C; c. 1-hexadecanoyl-glycerol - Phosphocholine, dicyclohexylcarbodiimide, dichloromethane, 25°C.
[0036] Step a: Dissolve 20 g of dodecylmercaptan and 10 g of triethylamine in 200 ml of dichloromethane, add a solution of 88 g of 2,2'-dithiobipyridine in 100 ml of dichloromethane with stirring in an ice bath , the reaction solution was stirred at 0° C. for 1 hour, then naturally rose to room temperature, and continued to stir for 24 hours. After the reaction was finished, the reaction solution was concentrated until a large amount of crystals appeared, and suction filtered. The filter cake was washed with 200 ml of n-hexane, and the combined filtrate was crystallized with 50 ml of glacial ether to obtain 25 g of compound 2 (light yellow solid), with a yield of 79%;
[0037] Step b: 15.5 grams of compound 2 and 5.3 grams of mercaptopro...
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