Hybridized peptide with 3S-tetrahydrochysene-beta-carboline-3-carboxylic acid as connecting arm, preparation method and application thereof
A carboline and carboxylic acid technology, applied in the field of hybrid peptides, can solve problems such as difficulty in detection, and achieve the effect of excellent thrombolytic activity
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1B
[0026] The preparation of embodiment 1Boc-Pro-Ala-Lys(Z)-OBz
[0027] 1) Preparation of Boc-Ala-Lys(Z)-Obzl
[0028] Dissolve 473mg (2.5mmol) Boc-Ala-OH in 10ml anhydrous tetrahydrofuran (THF), add 10ml 338mg (2.5mmol) N-hydroxybenzotriazole (HOBt) and 619mg (3mmol) dicyclohexyl Anhydrous tetrahydrofuran (THF) solution of carbonyldiimide (DCC). The reaction mixture was stirred in an ice bath for 20 minutes to obtain the corresponding active ester solution for use.
[0029]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...
Embodiment 2B
[0035] Embodiment 2Boc-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0036] 1) Preparation of HCl Pro-Ala-Lys(Z)-OBzl
[0037] A mixture of 1.596g (2.5mmol) Boc-Pro-Ala-Lys(Z)-OBzl and 15ml hydrogen chloride-ethyl acetate solution (4N) was stirred for 1 hour under ice-bath conditions, 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 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.
[0038] 2) Preparation of Boc-Arg(NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0039] 798mg (2.5mmol) Boc-Arg (NO 2 )-OH was dissolved in 10ml of anhydrous THF, and 10ml of anhydrous THF solution of 338mg (2.5mmol) HOBt and 619mg (3mmol) of DCC was added under ice cool...
Embodiment 3B
[0041] Embodiment 3Boc-Ala-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0042] 1) Preparation of HCl Arg (NO 2 )-Pro-Ala-Lys(Z)-OBzl
[0043] 2.099g (2.5mmol) Boc-Arg (NO 2 )-Pro-Ala-Lys(Z)-OBzl and 15ml of hydrogen chloride-ethyl acetate solution (4N) was stirred for 1 hour under ice-bath conditions, 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.
[0044] 2) Boc-Ala-Arg (NO 2 Preparation of )-Pro-Ala-Lys(Z)-OBzl
[0045] Dissolve 473mg (2.5mmol) of Boc-Ala-OH in 10ml of anhydrous THF, and add 10ml of anhydrous THF solution containing 338mg (2.5mmol) of HOBt and 619...
PUM
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com