Saturated fatty chain alcohol Glu-Asp-Gly tripeptide ester, synthetic method and application thereof
A technology of glu-asp-gly and aliphatic chain alcohol, applied in the directions of tripeptide components, non-active components of polymer compounds, peptides, etc., can solve the problem of poor water solubility of cyclosporin A, unsatisfactory dosage form or efficacy, and nephrotoxicity. Strong and other problems, to achieve the effect of excellent immunosuppressive effect
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Embodiment 1B
[0029] Example 1Boc-Gly-OCH 2 (CH 2 ) 6 CH 3 preparation of
[0030] 1.00 g (5.71 mmol) of Boc-Gly was dissolved in 20 ml of anhydrous THF, and 0.77 g (5.71 mmol) of N-hydroxybenzotriazole (HOBt) was added to the resulting solution under ice cooling to dissolve completely. After 10 minutes, 1.41 g (6.85 mmol) of dicyclohexylcarbodiimide (DCC) was added to obtain a reaction solution (I). Add 0.74g (5.71mmol) fatty alcohol CH under ice bath 3 (CH 2 ) 6 CH 2 OH was suspended in 20ml of anhydrous THF, and then 1ml of N-methylmorpholine (NMM) was added to adjust the pH to 8-9. Stir for 35 minutes to obtain reaction solution (II). The reaction solution (I) was added to the reaction solution (II) under ice-cooling, first stirred under ice-cooling for 1 h, then stirred at room temperature for 12 h, TLC (chloroform / methanol, 10:1) showed that Boc-Lys (Z) disappeared. Dicyclohexylurea (DCU) was filtered off and THF was removed under reduced pressure. The residue was dissolved...
Embodiment 2B
[0031] Example 2Boc-Gly-OCH 2 (CH 2 ) 8 CH 3 preparation of
[0032] According to the method of embodiment 1 by 1.00g (5.71mmol) Boc-Gly and 0.90g (5.71mmol) CH 3 (CH 2 ) 8 CH 2 OH yielded 1.64 g (91%) of the title compound as a colorless oil ESI-MS (m / z): 316 [M+H] + .
Embodiment 3B
[0033] Example 3Boc-Gly-OCH 2 (CH 2 ) 10 CH 3 preparation of
[0034] According to the method of embodiment 1 by 1.00g (5.71mmol) Boc-Gly and 1.06g (5.71mmol) CH 3 (CH 2 ) 10 CH 2 OH yielded 1.77 g (90%) of the title compound as a colorless oil. ESI-MS(m / z): 344[M+H] + .
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