50784-07-1Relevant articles and documents
Aza11-membered ring compound, preparation method and application thereof, and medicine containing aza11-membered ring compound
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Paragraph 0100; 0105-0107, (2021/01/15)
The invention discloses an aza 11-membered ring compound haveing the following structural general formula shown in the specification, and also provides a method for preparing the compound. The methodcomprises the following steps of: under the condition of argon, by taking methylbenzene as a solvent, coordinating a tri(dibenzylidene acetone)dipalladium-chloroform adduct with a (4,5-bis(diphenylphosphine)-9,9-dimethylxanthene)phosphine ligand; stirring, adding a substrate 1 and a substrate 2 after the solution turns yellow from red, and carrying out a reaction to obtain a final product 3 afterthe reaction is finished. The invention also discloses application of the compound and a medicine containing the compound. According to the invention, the exploration of the compound with the middle ring structure is further deeply carried out, the compound with the middle ring structure also has pharmaceutical activity, the preparation method capable of expanding production and large-scale production is provided, the adopted reaction substrate raw materials are very easy to obtain, the reaction conditions of the preparation method are easy to realize, the reaction time is shortened to the maximum extent, and high yield can be obtained.
Synthesis, anti-varicella-zoster virus and anti-cytomegalovirus activity of quinazoline-2,4-diones containing isoxazolidine and phosphonate substructures
Piotrowska, Dorota G.,Andrei, Graciela,Schols, Dominique,Snoeck, Robert,?ysakowska, Magdalena
, p. 84 - 100 (2016/10/25)
Cycloadditions of N-substituted C-(diethoxyphosphoryl)nitrones to N-allylated quinazoline-2,4-diones functionalized at N3 with substituted benzoyl or benzyl groups proceeded with moderate to good diastereoselectivities (d.e. 28–68%). The synthesized isoxazolidine phosphonates were assessed for the antiviral activity against a broad range of DNA and RNA viruses. Compounds trans-13c, cis-13c/trans-13c (86:14), cis-15b/trans-15b (87:13) and trans-15d/cis-15d (95:5) exhibited the highest activity toward both TK+and TK?VZV strains (mean EC50values in the range of 3.0–8.7?μM). The EC50's for isoxazolidines trans-12a, cis-12a, cis-13a, trans-13d, cis-15a/trans-15a (50:50) ranged between 6.9 and 8.5?μM for VZV TK+strain and between 10.7 and 13.2?μM for VZV TK–strain. The isoxazolidine phosphonates cis-15/trans-15 having benzyl substituents both at N3 of the quinazoline-2,4-dione skeleton and at N2 of the isoxazolidine ring displayed some anti-cytomegalovirus potency but at the same time showed significant cytostatic activity for human embryonic lung fibroblasts (used to carry out the antiviral assays) as well as for other cell lines (i.e. CEM, L1210, HeLa and HMEC-1).
PYRIMIDO [4,5-B]QUINOLINE-4,5 (3H,10H)-DIONES AS NONSENSE MUTATION SUPPRESSORS
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Page/Page column 15; 16, (2014/07/07)
The invention relates to compound of the formula (I); or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.