- Aza11-membered ring compound, preparation method and application thereof, and medicine containing aza11-membered ring compound
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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.
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Paragraph 0100; 0105-0107
(2021/01/15)
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- One-Pot Total Synthesis of Evodiamine and Its Analogues through a Continuous Biscyclization Reaction
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The one-pot total synthesis of evodiamine and its analogues is achieved using a three-component reaction. Through continuous biscyclization, various readily available substrates with good functional group tolerance were easily incorporated into biologically active quinazolinocarboline backbones. The use of triethoxymethane as a cosolvent was crucial for this quick and straightforward transformation.
- Wang, Zi-Xuan,Xiang, Jia-Chen,Wang, Miao,Ma, Jin-Tian,Wu, Yan-Dong,Wu, An-Xin
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supporting information
p. 6380 - 6383
(2018/10/20)
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- Synthesis, anti-varicella-zoster virus and anti-cytomegalovirus activity of quinazoline-2,4-diones containing isoxazolidine and phosphonate substructures
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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).
- Piotrowska, Dorota G.,Andrei, Graciela,Schols, Dominique,Snoeck, Robert,?ysakowska, Magdalena
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- Chemoselective oxidation of 1-alkenylisatins with m-chloroperbenzoic acid. Synthesis of new derivatives of isatoic anhydride
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Oxidation of alkyl- and alkenylisatins with m-chloroperbenzoic acid proceeds with high chemoselectivity leading to the formation of 1-substituted isatoic anhydrides (benzo[d][1,3]oxazine-2,4-diones) without epoxidation of the double bond of the alkenyl su
- Bogdanov,Sadykov,Musin,Khamatgalimov,Krivolapov,Dobrynin,Mironov
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p. 2030 - 2036
(2015/10/29)
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- PYRIMIDO [4,5-B]QUINOLINE-4,5 (3H,10H)-DIONES AS NONSENSE MUTATION SUPPRESSORS
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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.
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Page/Page column 15; 16
(2014/07/07)
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- RETRACTED ARTICLE: Novel 2-aminobenzamides as potential orally active antithrombotic agents
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In an effort to develop potent antithrombotic agents, a series of novel 2-aminobenzamide derivatives were synthesized and screened for their in vivo antithrombotic activity. Among the 23 compounds tested, compound (8g) showed the most promising antithrombotic activity, which was comparable with clinically used aspirin or warfarin, but at variance with these standard drugs, 8g did not exhibit the increased bleeding time, suggesting its potential as a novel antithrombotic agent.
- Verma, Amit,Giridhar, Rajani,Kanhed, Ashish,Sinha, Anshuman,Modh, Pratik,Yadav, Mange R.
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supporting information
p. 32 - 36
(2013/03/13)
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- Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT
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A library of 1,4-benzodiazepines has been synthesised and evaluated for activity against Trypanosoma brucei, a causative parasite of Human African Trypanosomiasis (HAT). The most potent of these derivatives has an MIC value of 0.97 μM. Herein we report the design, synthesis and biological evaluation of the abovementioned compounds.
- Clark, Rachel L.,Clements, Carol J.,Barrett, Michael P.,MacKay, Simon P.,Rathnam, Rajendra P.,Owusu-Dapaah, George,Spencer, John,Huggan, Judith K.
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p. 6019 - 6033
(2012/11/07)
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- Synthesis of N-substituted 2-[(1E)-alkenyl]-4-(1H)-quinolone derivatives as antimycobacterial agents against non-tubercular mycobacteria
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In an effort to improve biological activities and to examine antimycobacterial-lipophilicity relationships of 2-[(1E)-alkenyl)]-4-(1H)- quinolones, we have synthesized a series of 30 quinolones by introducing several alkyl groups, an alkenyl and an alkynyl group at N-1. All synthetic compounds were first tested in vitro against Mycobacterium smegmatis and the most active compounds (MIC values ～3.0-7.0 μM) were further examined against three other rapidly growing strains of mycobacteria using a microtiter broth dilution assay. The Clog P values of the synthetic compounds were calculated to provide an estimate of their lipophilicity. Compounds 18e, 19a and 19b displayed the most potent inhibitory effect against M. smegmatis mc2155 with an MIC value of ～1.5 μM, which was twenty fold and thirteen fold more potent than isoniazid and ethambutol, respectively. On the other hand, compounds 17e, 18e and 19a were most active against Mycobacterium fortuitum and Mycobacterium phlei with an MIC value of ～3.0 μM. In the human diploid embryonic lung cell line MRC-5 cytotoxicity assay, the derivatives showed moderate to strong cytotoxic activity. Although the antimycobacterial activity of our synthetic compounds could not be correlated with the calculated log P values, an increase in lipophilicity enhances the antimycobacterial activity and C 13-C15 total chain length at positions 1 and 2 is required to achieve optimal inhibitory effect against the test strains.
- Wube, Abraham A.,Bucar, Franz,Hochfellner, Christina,Blunder, Martina,Bauer, Rudolf,Hüfner, Antje
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experimental part
p. 2091 - 2101
(2011/06/21)
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- 1,3-dipolar cycloaddition-decarboxylation reactions of an azomethine ylide with isatoic anhydrides: Formation of novel benzodiazepinones
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A nonstabilized azomethine ylide reacts with a wide range of substituted isatoic anhydrides to afford novel 1,3-benzodiazepin-5-one derivatives, which are generally isolated in high yield. The transformations involve 1,3-dipolar cycloaddition reactions of the ylide with the anhydrides to give transient, and in a representative case spectroscopically observable, oxazolidine intermediates that undergo ring-opening-decarboxylation-ringclosing reaction cascades to yield the 1,3-benzodiazepin-5-one products.
- D'Souza, Asha M.,Spiccia, Nadia,Basutto, Jose,Jokisz, Pawel,Wong, Leon S.-M.,Meyer, Adam G.,Holmes, Andrew B.,White, Jonathan M.,Ryan, John H.
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supporting information; experimental part
p. 486 - 489
(2011/03/23)
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