Borneol ester derivative of carboxylic acid nonsteraidal anti-inflammatory medicaments as well as preparation method and application of borneol ester derivative
A non-steroidal anti-inflammatory drug, borneol technology, applied in the field of medicine, can solve problems such as adverse drug reactions, liver first-pass effect, and inability to maintain a constant blood drug concentration, achieve good transdermal absorption characteristics, and avoid common side effects Effect
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Embodiment 1
[0018] Embodiment 1: the synthesis of naproxenbornyl ester
[0019] In a 250 mL round bottom flask, add 10.0 g of naproxen, 10.1 g of borneol, 17.9 g of DCC, 300 mg of 4-dimethylaminopyridine (DMAP), and react at 110°C-120°C for 24 hours. The reaction mixture was filtered with a funnel to remove the milky white solid in the mixture. Take the filtrate and add 200ml of pure water to mix it, put it in a separatory funnel, shake it for 3 minutes, let it stand for liquid separation, and keep the upper layer solution. Then get 200ml ethyl acetate to extract the above solution, get the upper organic phase and pour it into a 250ml Erlenmeyer flask, clean the organic solution with 20% sodium carbonate solution with 150ml concentration, and then place it in a separatory funnel for liquid separation , remove the lower aqueous phase. Then take out the remaining organic phase liquid, wash it once with about 150ml sodium chloride solution, wash the solution until neutral, and finally wash...
Embodiment 2
[0020] Embodiment 2: the synthesis of ketoprofen bornyl ester
[0021] In a 250mL round bottom flask, add 10g of ketoprofen, 9.1g of borneol, 16.2g of DCC, 300mg of DMAP, and react at 110°C-120°C for 24h. The reaction mixture was filtered with a funnel to remove the milky white solid in the mixture. Take the filtrate and add 200ml of pure water to mix it, put it in a separatory funnel, shake it for 3 minutes, let it stand for liquid separation, and keep the upper layer solution. Then get 200ml ethyl acetate to extract the above solution, get the upper organic phase and pour it into a 250ml Erlenmeyer flask, clean the organic solution with 20% sodium carbonate solution with 150ml concentration, and then place it in a separatory funnel for liquid separation , remove the lower aqueous phase. Then take out the remaining organic phase liquid, wash it once with about 150ml sodium chloride solution, wash the solution until neutral, and finally wash it again with pure water. The cl...
Embodiment 3
[0022] Embodiment 3: the synthesis of bornyl flufenamate
[0023] In a 250mL round bottom flask, add 10g of flufenamic acid, 8.2g of borneol, 14.7g of DCC, 300mg of DMAP, and react at 110°C-120°C for 24h. The reaction mixture was filtered with a funnel to remove the milky white solid in the mixture. Take the filtrate and add 200ml of pure water to mix it, put it in a separatory funnel, shake it for 3 minutes, let it stand for liquid separation, and keep the upper layer solution. Then get 200ml ethyl acetate to extract the above solution, get the upper organic phase and pour it into a 250ml Erlenmeyer flask, clean the organic solution with 20% sodium carbonate solution with 150ml concentration, and then place it in a separatory funnel for liquid separation , remove the lower aqueous phase. After taking out the remaining organic phase liquid, wash it once with about 150ml of sodium chloride solution until the solution is neutral, and finally wash it again with pure water. The...
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