Hybrid peptide using 3S-tetrahydro-beta-carboline-3-carboxylic acid as connecting arm, and preparation method and application thereof
A carboline, general formula technology, applied in the field of hybrid peptides, can solve problems such as difficulty in detection, and achieve the effect of excellent thrombolytic activity
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Embodiment 1
[0023] Embodiment 1 Preparation of Boc-Pro-Ala-Lys(Z)-OBz
[0024] 1) Preparation of Boc-Ala-Lys(Z)-OBzl
[0025] Dissolve 473mg (2.5mmol) Boc-Ala in 10ml anhydrous anhydrous tetrahydrofuran (THF), add 10ml containing 338mg (2.5mmol) N-hydroxybenzotriazole (HOBt) and 619mg (3mmol) bicyclic Hexylcarbodiimide (DCC) in anhydrous THF. The reaction mixture was stirred in an ice bath for 20 minutes to obtain the corresponding active ester solution for use.
[0026] 936mg (2.3mmol) HCl·Lys(Z)-OBzl and 232mg (2.3mmol) N-methylmorpholine were first miscible with 6ml of anhydrous THF, and then with the active ester solution to be used above. The resulting reaction mixture was reacted at room temperature for 24 hours. TLC (developer CHCl3:MeOH=20:1) showed that HCl·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 was filtered off. The filtrate was washed successively...
Embodiment 2
[0032] Example 2 Boc-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0033] 1) Preparation of HCl Pro-Ala-Lys(Z)-OBzl
[0034] A mixture of 1.596g (2.5mmol) Boc-Pro-Ala-Lys(Z)-OBzl in 15ml of ethyl acetate (4N) containing hydrogen chloride was stirred under ice bath for 1 hour, TLC (developing agent CHCl 3 :MeOH=20:1) showed that Boc-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 triturated with anhydrous ether 5 times. The obtained title compound was directly used in the next reaction.
[0035] 2) Preparation of Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0036] 798mg (2.5mmol) Boc-Arg (NO 2 ) was dissolved in 10ml of anhydrous THF, and 10ml of anhydrous THF solution containing 338mg (2.5mmol) of HOBt and 619mg (3mmol) of DCC was added under ice cooling. The reaction mixture was stirred in ice bath for 20 minutes to obtain the cor...
Embodiment 3
[0038] Example 3 Boc-Ala-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0039] 1) Preparation of HCl Arg (NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0040] 2.099g (2.5mmol) Boc-Arg (NO 2 )-Pro-Ala-Lys(Z)-OBzl and 15ml of hydrogen chloride-containing ethyl acetate (4N) mixture was stirred under ice bath for 1 hour, TLC (developing agent CHCl 3 : MeOH=10:1) shows that 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, rubbed with a plastic shovel, and poured out of anhydrous ether, repeated 5 times. The obtained title compound was directly used in the next reaction.
[0041] 2) Boc-Ala-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0042] Dissolve 473mg (2.5mmol) of Boc-Ala in 10ml of anhydrous THF, add 10ml of anhydrous THF solution containing 338mg (2.5mmol) of HOBt and 619mg (3mmol)...
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