Saturated fatty chain alcohol His-Gly-AA tripeptide ester, synthetic method and application thereof
A his-gly-aa, aliphatic chain alcohol technology, applied in the field of biomedicine, can solve the problems of poor water solubility of cyclosporin A, unsatisfactory dosage form or efficacy, strong nephrotoxicity, etc., and achieve excellent immunosuppressive effect.
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Embodiment 1
[0039] Example 1 Preparation of Boc-Glu(OBzl)-OCH 2 (CH 2 ) 6 CH 3
[0040] 1.00g (2.96mmol) Boc-Glu (OBzl) was dissolved in 20ml of anhydrous THF, and 0.39g (2.96mmol) N-hydroxybenzotriazole (HOBt) was added to the resulting solution under ice cooling, and completely dissolve. After 10 minutes 0.74 g (3.55 mmol) of dicyclohexylcarbodiimide (DCC) were added. The reaction liquid (I) was obtained. 0.39g (2.96mmol) fatty alcohol CH 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, and then stirred at room temperature for 12 h, TLC (chloroform / methanol, 10:1) showed that Boc-Glu (OBzl) disappeared. Dicyclohexylurea (DCU) was filtered off and THF was removed under reduced pressure. The residue was dissolved ...
Embodiment 2
[0041] Example 2 Preparation of Boc-Glu(OBzl)-OCH 2 (CH 2 ) 8 CH 3
[0042] According to the method of embodiment 1 by 1.00g (2.96mmol) Boc-Glu (OBzl) and 0.47g (2.96mmol) CH 3 (CH 2 ) 8 CH 2 OH yielded 1.37 g (97%) of the title compound as a colorless oil.
[0043] ESI-MS(m / z): 478[M+H] + , [α] 20 D =-11.6 (c=1.0, CH 3 OH).
Embodiment 3
[0044] Example 3 Preparation of Boc-Glu(OBzl)-OCH 2 (CH 2 ) 10 CH 3
[0045] According to the method of embodiment 1 by 1.00g (2.96mmol) Boc-Glu (OBzl) and 0.55g (2.96mmol) CH 3 (CH 2 ) 10 CH 2 OH yielded 1.46 g (98%) of the title compound as a colorless oil.
[0046] ESI-MS(m / z): 506[M+H] + , [α] 20 D =-11.5 (c=1.0, CH 3 OH).
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