Taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition
A kinase inhibitor, paclitaxel technology, applied in the field of chemical medicine, can solve problems such as the ineffectiveness of anticancer agents, and achieve the effects of reducing clinical dosage, reducing toxic side effects, and good anticancer efficacy
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Example Embodiment
[0018] Example 1 1-Phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)pyridin-2-ylamino ) Synthesis of Pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
[0019]
[0020] Step 1 Synthesis of 2-amino-5-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)pyridine
[0021]
[0022] Weigh 2.24g 5-methyl-2,5-diazabicyclo[2.2.1]heptane into the reaction flask, add 50ml of DMF / water mixed solvent with a volume ratio of 1:1 to dissolve, add 0.52g 2- Amino-5-chloropyridine was reacted at 100°C for 8 hours. After the reaction was completed, 20ml of water was added, extracted with ethyl acetate, the organic phase was dried with anhydrous sodium sulfate, filtered, and spin-dried to obtain the title compound.
[0023] LC-MS m / z:[M+H] + =205.
[0024] Step 2 1-Phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl)pyridin-2-ylamino) Synthesis of Pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
[0025] Using the product obtained in step 1, 2,4-dichloro-5-nitropyrimidine, and methylamine hydroc...
Example Embodiment
[0028] Example 2 1-Phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)pyridin-2-ylamino ) Synthesis of Pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione hydrobromide
[0029]
[0030] Weigh 15g of the compound of Example 1 in a reaction flask, add 50ml of dichloromethane to dissolve, add 5.9g of hydrobromic acid, heat to 45°C and stir for 0.5h, after cooling to room temperature, the solvent is evaporated under reduced pressure to obtain the title compound.
Example Embodiment
[0031] Experimental example 1 stability experiment
[0032] Weigh 4 parts of 1g of the compounds of Examples 1 to 3, and place them for 1 month under the conditions of illumination 4500Lx, RH70% at 75°C, RH70% at 60°C, and RH70% at room temperature. The experimental results are shown in Table 1.
[0033] Table 1
[0034]
[0035] The experimental results show that the compounds of Examples 2 and 3 of the present invention have very high stability.
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