Podophyllotoxin phospholipid compound as well as pharmaceutical composition and application of podophyllotoxin phospholipid compound
A technology of phospholipid compound and podophyllotoxin, which is applied in the field of medicine, can solve the problems of leakage of drugs and difficulty in exerting efficacy of drugs, and achieve the effect of low toxicity and side effects.
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Embodiment 1
[0112] Synthesis of bis(podophyllotoxin-4-succinic acid) phosphatidylcholine (see the synthetic route figure 1 )
[0113] Podophyllotoxin 0.5g, succinic anhydride 3g, DMAP 0.1g, triethylamine 3g, add dichloromethane as reaction solvent, reflux reaction for 12h; wash with dilute hydrochloric acid three times, filter dilute hydrochloric acid layer, take filter cake; add methanol to dissolve, Place at 4°C for 12 hours, filter, take the filter cake, and dry to obtain the intermediate product podophyllotoxin-4-succinic acid monoester.
[0114] Podophyllotoxin-4-succinic acid monoester 0.6g, add CDI1.2g, dichloromethane is reaction solvent, add GPC0.4g and DBU1g to react at room temperature, the obtained reaction solution is purified by column chromatography, and the product bis(podophyllotoxin - 4-succinic acid) phosphatidylcholine (MW1249.4) 0.28g.
[0115] For the NMR spectrum of the compound, see figure 2 , 1 HNMR (500MHz, (CD 3 ) 2 SO): δ6.86(2H,s,8-H),6.56(2H,s,5-H),6.4...
Embodiment 2
[0118] Synthesis of bis(4'-desmethyl epipodophyllotoxin-4-succinic acid) phosphatidylcholine (see the synthetic route Figure 4 )
[0119] 0.5g of 4'-desmethyl epipodophyllotoxin, 3g of succinic anhydride, 0.1g of DMAP, 3g of triethylamine, add dichloromethane as the reaction solvent, react at 45°C for 48h; wash with dilute hydrochloric acid three times, filter the dilute hydrochloric acid layer, Take the filter cake; add methanol to dissolve, place at 4°C for 12h, filter, take the filter cake, and dry to obtain the intermediate product 4'-desmethyl epipodophyllotoxin-4-succinic acid monoester.
[0120] Add 0.5g of 4'-desmethyl epipodophyllotoxin-4-succinic acid monoester, add 1.0g of CDI, dichloromethane as the reaction solvent, add 0.3g of GPC and 0.8g of DBU to react at room temperature, and the resulting reaction solution is passed through column chromatography After purification, 0.24 g of the product bis(4'-desmethylepipodophyllotoxin-4-succinic acid) phosphatidylcholine ...
Embodiment 3
[0124] Synthesis of bis(podophyllotoxin-4-succinic acid) phosphatidylethanolamine (see the synthetic route Figure 5 )
[0125] Take 0.5g of 3-(4-methoxybenzyloxy)propane-1,2-diol, 0.5g of succinic anhydride, 0.1g of DMAP, 0.5g of triethylamine, add dichloromethane as the reaction solvent, add reflux React, react for 12 hours; wash with dilute hydrochloric acid three times, filter the dilute hydrochloric acid layer, and take the filter cake; add 0.5g of CDI, add dichloromethane as the reaction solvent, and react at room temperature for 3h; add 0.5g of podophyllotoxin, DBU0.5g, and react at room temperature 12h, spin dry the solvent; add dilute acetic acid, react at room temperature for 6h, remove the solvent; add phosphorus oxychloride 0.5g, triethylamine 0.5g, add dichloromethane as the reaction solvent, react at 10°C for 24h, spin dry the solvent; Add 0.5 g of aminoethanol, 0.3 g of triethylamine, add dichloromethane as the reaction solvent, react at 10°C for 24 hours, and ...
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