A kind of antiviral medicine and preparation method thereof
A drug and viral technology, which is applied to the ester of peramivir and plerixafor-N-alkanoic acid, the derivative ester of peramivir, and the preparation field of the antiviral drug, which can prolong the survival time, The effect of increased mortality protection
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Embodiment 1
[0046] Example 1 (1S,2S,3R,4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-valerate
[0047]
[0048] (1) (1S,2S,3R,4R)-2-Hydroxy-3-[(1S)-1-acetamido-2-ethyl]butyl-4-diBoc-guanidinocyclopenta-1- Benzyl carboxylate
[0049]
[0050] Add 32.8g (100mmol) of peramivir, 21.3g (112mmol) of p-toluenesulfonic acid, 54.1g (500mmol) of benzyl alcohol, and add 500mL of toluene to reflux for 24 hours (using a water separator). After the reaction is completed, Add ethyl acetate to freeze and crystallize, suction filter, wash with ethyl acetate, add 200mL tetrahydrofuran to the filter cake to dissolve, add 30.3g (300mol) of triethylamine, add 109.1g (500mmol) of di-tert-butyl dicarbonate (BOC anhydride ), stirred at room temperature for 24 hours, added 400 mL of dichloromethane after the reaction was completed, adjusted the pH to 2-3 with hydroch...
Embodiment 2
[0066] Example 2 (1S,2S,3R,4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-octadecanoate
[0067]
[0068] Prepared as in Example 1, replacing ethyl 5-bromopentanoate in step (3) with ethyl 18-bromo-octadecanoate to obtain the target compound; high-resolution mass spectrum (+ESI, m / z): 1096.6419 [M+H] + .
Embodiment 3
[0069]Example 3 (1S,2S,3R,4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-methyl-phenyl-valerate
[0070]
[0071] Prepared as in Example 1, replacing ethyl 5-bromovalerate in step (3) with p-bromomethyl-ethyl valerate to obtain the target compound; high-resolution mass spectrum (+ESI, m / z): 1004.4098 [M+H] + .
[0072] The selectivity index and the death protection rate of the peramivir derivative ester provided by the present invention are further compared and illustrated by the test examples below.
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