Compounds with thrombolytic activities and preparation methods and applications thereof
A compound, the technology of suppository activity, applied in the field of medicinal chemistry
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Embodiment 2
[0042] Example 2 Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl preparation
[0043] 1) Preparation of HCl·Pro-Ala-Lys(Z)-OBzl
[0044] A mixture of 1.596g (2.5mmol) Boc-Pro-Ala-Lys(Z)-OBzl and 15ml of hydrogen chloride-ethyl acetate solution (4N) was stirred at room temperature for 3 hours, TLC (developing solvent chloroform: methanol = 10:1) showed Boc-Pro-Ala-Lys(Z)-OBzl disappeared. The reaction solution was drained by a water pump, ethyl acetate was added, and the reaction solution was drained by a water pump. Repeat 5 times. The residue was soaked and washed with anhydrous ether, and the reaction solution was drained again with a water pump, repeated 5 times. The obtained title compound was directly used in the next reaction.
[0045] 2) Preparation of Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0046] Add 798mg (2.5mmol) Boc-Arg(NO 2 )-OH was dissolved in 10ml anhydrous THF, and 10ml 338mg (2.5mmol) HOBt and 619mg (3mmol) DCC in anhydrous THF were added to it under ice bath. The reaction mixt...
Embodiment 3
[0050] Example 3 Boc-Ala-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl preparation
[0051] 1) Preparation of HClArg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0052] Add 2.099g (2.5mmol) Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl and 15ml hydrogen chloride-ethyl acetate (4N) mixture was stirred at room temperature for 3 hours, TLC (developing solvent chloroform: methanol = 10:1) showed Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl disappeared. Drain the reaction solution with a water pump, add anhydrous ether, and drain the reaction solution with a water pump again, repeating 5 times. The residue was soaked and washed with anhydrous ether, washed with a plastic spatula, and the anhydrous ether was poured out, repeated 5 times. The obtained title compound was directly used in the next reaction.
[0053] 2) Preparation of Boc-Ala-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0054] Dissolve 473 mg (2.5 mmol) of Boc-Ala-OH in 10 ml of anhydrous THF, and add 10 ml of an anhydrous THF solution of 338 mg (2.5 mmol) HOBt and 619 mg (3 mmol) DCC in ...
Embodiment 4
[0058] Example 4 Boc-Gly-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl preparation
[0059] 1) Preparation of Boc-Gly-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0060] Dissolve 438 mg (2.5 mmol) of Boc-Gly-OH in 10 ml of anhydrous THF, and add 10 ml of an anhydrous THF solution of 338 mg (2.5 mmol) HOBt and 619 mg (3 mmol) DCC under ice bath. The reaction mixture was stirred in an ice bath for 20 minutes to obtain the corresponding active ester solution, which was set aside.
[0061] Add 2.025g (2.3mmol) HCl·Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl and 232mg (2.3mmol) of N-methylmorpholine are first miscible with 6ml of anhydrous THF, and then miscible with the active ester solution to be used above. The resulting reaction mixture was reacted at room temperature for 24 hours. TLC (developer chloroform: methanol = 10:1) showed HCl·Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl disappeared. The reaction mixture was concentrated to dryness under reduced pressure, the residue was dissolved in ethyl acetate, and the insoluble matter wa...
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