Prodrug based on intestinal OCTN2 carrier protein design and preparation method thereof
A prodrug and pharmaceutical technology, applied in the field of medicine, can solve the problems of low oral bioavailability and poor permeability, and achieve the effect of increasing compliance and reducing risks
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[0039] Example 14-Preparation of benzyl L-carnitine
[0040] 5.3 g (32.9 mmol) of L-carnitine and 4.50 g (26.3 mmol) of bromide were dissolved in 20 mL of DMF, heated to reflux at 140° C. for 2 h, and concentrated under reduced pressure to obtain 5.53 g of white solid with a yield of 83.3%. ESI-MS[M+H] + (m / z): 252 (Intermediate 1).
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[0041] Example 22-Butyrate-4-benzyl-L-carnitine preparation
[0042] Dissolve 1g (3.9mmol) of intermediate and 0.48g (4.8mmol) of succinic anhydride in 10mL of DMF, add 2 drops of triethylamine at 0°C, and vacuum with nitrogen after the drops. The reaction is complete after 2h, no need for reaction The processing proceeds directly to the next step. ESI-MS[M+H] + (m / z): 352 (Intermediate 2).
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[0043] Example 32 Preparation of hexanoyl-4-benzyl-L-carnitine
[0044] Dissolve 1g (3.9mmol) of intermediate and 0.59g (4.8mmol) of adipic anhydride in 10mL of DMF, add 2 drops of triethylamine at 0℃, and vacuum and protect with nitrogen. After 2h, the reaction is complete and the reaction does not require treatment. Go directly to the next step. ESI-MS[M+H] + (m / z): 380 (Intermediate 3).
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