Lys and oligopeptide-modified curcumin derivatives, and synthesis and medical application thereof
A technology of -ala-gly-asp-val and -arg-gly-asp-val, applied in the direction of medical preparations containing active ingredients, cyclic peptide ingredients, drug combinations, etc., can solve the problem that curcumin has no thrombolytic activity, etc. question
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Embodiment 1
[0058] Embodiment 1 prepares Boc-Pro-Ala-Lys (Boc)
[0059] 1) Preparation of Boc-Pro-Ala
[0060] 1.075g (5.0mmol) of Boc-Pro was dissolved in 20mL of anhydrous THF, and 0.637g (5mmol) of N-hydroxysuccinimide (HOSu) was added to the solution under ice cooling, and completely dissolved. Under ice-cooling, 1.236 g (6.0 mmol) of dicyclohexylcarbodiimide (DCC) dissolved in a small amount of anhydrous THF was added to the reaction solution. Stir at room temperature for 7 h, and monitor the disappearance of Boc-Pro by TLC (petroleum ether / ethyl acetate, 3:1). Dicyclohexylurea (DCU) was filtered off, and the filtrate was concentrated under reduced pressure to remove THF. The residue was dissolved with ethyl acetate, and the solution was successively washed with saturated NaHCO 3 After washing with aqueous solution and saturated NaCl aqueous solution, the ethyl acetate layer was concentrated to dryness under reduced pressure, the residue was dissolved by adding an appropriate amou...
Embodiment 2
[0065] Example 2 Preparation of Arg-Gly-Asp(OBzl)-Val-OBzl
[0066] 1) Preparation of Boc-Arg-Gly-OBzl
[0067] According to the preparation method of item 2) in Example 1, 1.600 g (5.0 mmol) Boc-Arg and 1.689 g (5.0 mmol) Gly-OBzl were reacted to obtain 2.26 g (97%) of the title compound as a pale yellow solid. ESI-MS(m / e): 421.7[M+H] + .
[0068] 2) Preparation of Boc-Arg-Gly
[0069] According to the preparation method in item 3) of Example 1, 1.630 g (3.5 mmol) of Boc-Arg-Gly-Obzl was hydrolyzed to obtain 1.236 g (94%) of the title compound as a colorless solid. ESI-MS(m / e): 331.3[M-H] - .
[0070] 3) Preparation of Boc-Asp(OBzl)-Val-OBzl
[0071] According to the preparation method of item 2) in Example 1, 2.871 g (97%) of the title compound was obtained as a colorless oil from 1.620 g (5.0 mmol) Boc-D (OBzl) and 1.607 g (5.0 mmol) Val-OBzl. ESI-MS(m / e): 512[M+H] + .
[0072] 4) Preparation of Asp(OBzl)-Val-OBzl
[0073] Dissolve 5.12g (10mmol) Boc-Asp(OBzl)-Val...
Embodiment 3
[0078] Example 3 Preparation of Ala-Gly-Asp(OBzl)-Val-OBzl
[0079] 1) Preparation of Boc-Ala-Gly-OBzl
[0080] According to the preparation method of item 2) in Example 1, 1.600 g (5.0 mmol) Boc-Ala and 1.689 g (5.0 mmol) Gly-OBzl were reacted to obtain 2.26 g (97%) of the title compound as a pale yellow solid. ESI-MS(m / e): 337[M+H] + .
[0081] 2) Preparation of Boc-Ala-Gly
[0082] According to the preparation method of item 3) in Example 1, 1.236 g (94%) of the title compound was hydrolyzed from 1.630 g (3.5 mmol) of Boc-R-G-OBzl as a colorless solid. ESI-MS(m / e): 245[M-H] - .
[0083] 3) Preparation of Boc-Asp(OBzl)-Val-OBzl
[0084] According to the preparation method of item 2) in Example 1, 2.871 g (97%) of the title compound were obtained from 1.620 g (5.0 mmol) Boc-Asp (OBzl) and 1.607 g (5.0 mmol) Val-OBzl as a colorless oil. ESI-MS(m / e): 512[M+H] + .
[0085] 4) Preparation of Asp(OBzl)-Val-OBzl
[0086] According to the preparation method in item 4) of E...
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