Combined antitumor drug, preparation method and applications thereof
A technology of anti-tumor drugs and combined drugs, which is applied in the field of anti-tumor drugs and preparations, can solve problems such as rapid release, and achieve the effects of inhibiting proliferation, inhibiting tumor growth, and inhibiting the formation of vascular lumens
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Example Embodiment
[0042] Example 1
[0043] Take butyric acid (51.7μL, 0.57mmol), CA4 (180mg, 0.57mmol), EDC·HCl (163mg, 0.855mmol), DMAP (76.6mg, 0.627mmol), DIEA (188.9μL, 1.14mmol) and dissolve in 4ml DCM After stirring overnight at room temperature, add ethyl acetate, use 5% citric acid, saturated NaHCO 3 Wash the organic phase with saturated brine, dry the organic phase with anhydrous sodium sulfate, filter, collect the filtrate and remove the solvent under reduced pressure; the solid is separated and purified by column chromatography (ethyl acetate:n-hexane=1:3) to obtain the target The product, butyric acid-CA4 conjugate compound 2 (280 mg, yield 93%).
[0044] Product of butyric acid-CA4 1 H NMR nuclear magnetic data and mass spectrum data are as follows:
[0045] 1 H NMR(400MHz, CDCl 3 ): δ1.00-1.04(t,3H),1.73-1.78(m,2H), 2.49-2.53(t,2H), 3.71(s,6H), 3.80(s,3H), 3.83(s,3H) ), 6.45-6.45 (d, 2H, J = 1.2), 6.51 (s, 2H), 6.83-6.85 (d, 1H, J = 8.4), 7.00-7.01 (d, 1H, J = 1.6), 7.10- 7.12(q,1H)....
Example Embodiment
[0047] Example 2
[0048] Take heptanoic acid (80.8μL, 0.57mmol), CA4 (180mg, 0.57mmol), EDC·HCl (163mg, 0.855mmol), DMAP (76.6mg, 0.627mmol), DIEA (188.9μL, 1.14mmol) and dissolve in 4mL DCM After stirring overnight at room temperature, add ethyl acetate, use 5% citric acid, saturated NaHCO 3 Wash the organic phase with saturated brine, dry the organic phase with anhydrous sodium sulfate, filter, collect the filtrate and remove the solvent under reduced pressure; the solid is separated and purified by column chromatography (ethyl acetate:n-hexane=1:3) to obtain the target The product, heptanoic acid-CA4 conjugate compound 3 (260 mg, yield 85%).
[0049] Product of heptanoic acid-CA4 1 H NMR nuclear magnetic data and mass spectrum data are as follows:
[0050] 1 H NMR(400MHz, CDCl 3 ): δ0.88-0.91(t,3H),1.26-1.41(m,6H),1.70-1.74(t,2H),2.51-2.54(t,2H),3.71(s,6H),3.80(s ,3H),3.84(s,3H),6.45-6.45(d,2H,J=1.6),6.51(s,2H),6.83-6.85(d,1H,J=8.4),7.00-7.00(d, 1H, J = 1.6), 7.10-7.12 (q, 1H)...
Example Embodiment
[0052] Example 3
[0053] The synthesis method of LNA-SN38 conjugate compound 4 refers to the synthesis of SN38 prodrug 7 in the patent document "7-ethyl-10-hydroxycamptothecin prodrug and its preparation method and application", the patent application number is 201410295432. X.
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.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap