A pleuromutilin derivative with amide side chain and its preparation and application
A technology for pleuromutilin and derivatives, which is applied in the fields of pleuromutilin derivatives and their preparation and application, can solve the problem of rare pleuromutilin antibacterial drug-resistant bacteria and the like, and achieve good in vitro antibacterial activity , low preparation cost, good water solubility
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Embodiment 1
[0115](1) Preparation of Intermediate I: Dissolve 10.0g (26.5mmol) pleuromutilin in 20ml pyridine and place in an ice bath; dissolve 5.6g (29.2mmol) p-toluenesulfonyl chloride in 10ml pyridine, then slowly add For the above-mentioned pleuromutilin pyridine solution, after stirring the mixture in an ice bath for 3 h, add 50 ml each of ice water and chloroform in turn, then transfer to a separatory funnel for shaking, and let it stand until it is separated; take the organic phase, Wash with 100ml of 4mol / L sulfuric acid, 100ml of saturated sodium bicarbonate solution, and 100ml of deionized water in sequence; after washing, the organic phase evaporates the organic solution under reduced pressure, adds 20ml of isopropanol to the remaining solid, heats and dissolves, and then let cool to precipitate A large amount of white powder was suction-filtered, and the filter residue was washed with isopropanol and dried to obtain intermediate I with the structure shown in formula 3, with a ...
Embodiment 2
[0119] Example 2 Synthesis of 22-O-(benzamido)acetylmurein (compound 1)
[0120] Take 1g (2.65mmol) of Intermediate III and dissolve it in 23ml of dichloromethane, get 0.73g (5.30mmol) of anhydrous potassium carbonate and add it to the reaction system; dissolve 0.41g (2.92mmol) of benzoyl chloride in a small amount of dichloromethane, Slowly add dropwise to the above reaction system under ice-bath conditions, then stir the mixture in ice-bath for 3 hours, then add 50ml each of ice water and chloroform in turn, then transfer to a separatory funnel for shaking, and let it stand for layering. The organic phase was washed twice with aqueous sodium chloride solution (15% w / v) and dried over anhydrous sodium sulfate, and the organic phase was taken; the obtained organic phase was evaporated to dryness to obtain a mixture, redissolved in dichloromethane, and added with 100- 200 mesh silica gel 2g was fully mixed, and after the solvent evaporated, the above-mentioned crude product-sil...
Embodiment 3
[0121] Example 3 Synthesis of 22-O-(3-methoxy-benzamido)acetyl muulin (compound 6)
[0122] Take 1g (2.65mmol) of Intermediate III and dissolve it in 23ml of dichloromethane, take 0.73g (5.30mmol) of anhydrous potassium carbonate and add it to the reaction system; dissolve 0.50g (2.92mmol) of 3-methoxy-benzoyl chloride in A small amount of dichloromethane was slowly added dropwise to the above reaction system under ice bath conditions, then the mixture was stirred in ice bath for 3 hours, then 50ml each of ice water and chloroform were added in turn, and then transferred to a separatory funnel for shaking, statically Leave it to separate layers, take its organic phase and wash twice with aqueous sodium chloride solution (15% w / v) and dry with anhydrous sodium sulfate, take the organic phase; the obtained organic phase is rotary evaporated to dryness to obtain the mixture, and the mixture is washed with dichloromethane Redissolve, add 2 g of 100-200 mesh silica gel and mix thor...
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