Salt and crystal form of egfr inhibitor, and composition and use thereof
US-2024352053-A1 · Oct 24, 2024 · US
US9023866B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9023866-B2 |
| Application number | US-201313892522-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 13, 2013 |
| Priority date | Dec 7, 2006 |
| Publication date | May 5, 2015 |
| Grant date | May 5, 2015 |
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2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na + form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
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What is claimed is: 1. A compound of 2-selenophene 4-quinolone having the following formulas IIb or IIc: wherein R 2 ′, R 3 ′ and R 4 ′ independently are H, (CH 2 ) n CH 3 , Y(CH 2 ) n CH 3 , or X, wherein n is an integer of 0-4, Y is O, and X is F, Cl, or Br; R 2 and R 5 independently are H, (CH 2 ) n CH 3 , or X, and R 3 and R 4 together is —Y(CH 2 ) n Y—, wherei…
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