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[thiobarbiturat99]

Коллеги, добрый день!
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C2(=S)NC(=O)C(C)=C(CC1=C(F)C=CC=C1Cl)N2
В бензольном кольце могут также стоять вместо атома фтора атом хлора и наоборот. по шестому положению вместо метила (который показан на схеме) может также стоять этил, изопропил, метокси, этокси и т.д. радикалы. В общем любые
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[Arkadii_Tarasevych]

Результаты запроса по скайфайндеру: выдало 5 структур (некоторый вариации в замещении), которые описаны в следующих статьях:

1. Synthesis and Biological Evaluation of 6-Substituted 5-Alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as Potent HIV-1 NNRTIs By Yu, Mingyan; Li, Zhenyu; Liu, Shuai; Fan, Erkang; Pannecouque, Christophe; De Clercq, Erik; Liu, Xinyong From ChemMedChem (2011), 6(5), 826-833. Language: English, Database: CAPLUS
A series of new 5-alkyl-2-phenylaminocarbonylmethylthiopyrimidin-4(3H)-ones bearing variously substituted arylmethyl moieties at the C6 position of the pyrimidine ring were synthesized and evaluated for anti-HIV activity in MT-4 cells. Most of these new congeners exhibited moderate to good activities against the wild-type virus, with EC50 values in the range of 1.40-0.19 μM. Among them, 2-[(4-cyanophenylamino)carbonylmethylthio]-6-(2-chloro-6-fluorobenzyl)-5-ethylpyrimidin-4(3H)-one 4 b6 (I) is one of the compds. endowed with the highest broad-spectrum HIV-1 inhibitory activity, with EC50 va...
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2. Synthesis of new derivatives of 5-alkyl-6-(2,6-dihalobenzyl)-2-(methylsulfanyl)pyrimidin-4(3H)-one and the features of their oxidation By Novakov, I. A.; Orlinson, B. S.; Navrotskii, M. B.; Eremiichuk, A. S.; Brunilina, L. L.; Gordeeva, E. A.; Gerasimov, E. N. From Russian Journal of Organic Chemistry (2010), 46(11), 1691-1694. Language: English, Database: CAPLUS
The synthesis and regioselective S-monomethylation of new 5-alkyl-6-(arylmethyl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-ones was investigated. Addnl., the oxidative degrdn. of these compds. on treatment with H2O2-AcOH was studied.
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3. The specific character of the reaction of derivatives of 2-thioxo-2,3-dihydropyrimidin-4(1H)-one with iodomethane and alkyl chloromethyl sulfides By Novakov, I. A.; Orlinson, B. S.; Nawrozkij, M. B.; Mai, A.; Artico, M.; Rotili, D.; Eremiychuk, A. S.; Gordeeva, E. A.; Brunilina, L. L.; Este, J. A. From Chemistry of Heterocyclic Compounds (New York, NY, United States) (2010), 46(2), 200-205. Language: English, Database: CAPLUS
The alkylation of 5-alkyl-6-(2,6-dihalobenzyl)-2-thioxo-2,3-dihydropyrimidin-4(1H)-ones with MeI, AllSCH2Cl, and MeSCH2Cl in the K2CO3-DMF, NaOMe-MeOH, and KOH-EtOH systems was studied. A hypothetical mechanism for the reaction is examd., and an explanation is proposed for the compn. of the reaction products. The presence of high anti-HIV-1 activity was established in the obtained derivs. of 2-{[(allylsulfanyl)Me]sulfanyl}pyrimidin-4(3H)-one.
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4. Efficient solid-phase synthesis of isocytosine derivatives By Novakov, I. A.; Orlinson, B. S.; Brunilin, R. V.; Nawrozkij, M. B.; Gordeeva, E. A.; Savel ev, E. N.; Gerasimov, E. N. From Chemistry of Heterocyclic Compounds (New York, NY, United States) (2009), 45(11), 1365-1369. Language: English, Database: CAPLUS
A solid-phase synthesis of novel 6-(arylmethyl)-5-methylisocytosines by immobilization of the corresponding 2-thiothymine on a Merrifield resin, subsequent oxidn. to the sulfone, and finally aminolysis under mild conditions was presented.
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5. 5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a Series of Anti-HIV-1 Agents of the Dihydro-alkoxy-benzyl-oxopyrimidine Family with Peculiar Structure-Activity Relationship Profile By Nawrozkij, Maxim B.; Rotili, Dante; Tarantino, Domenico; Botta, Giorgia; Eremiychuk, Alexandre S.; Musmuca, Ira; Ragno, Rino; Samuele, Alberta; Zanoli, Samantha; Armand-Ugon, Mercedes; et alFrom Journal of Medicinal Chemistry (2008), 51(15), 4641-4652. Language: English, Database: CAPLUS
A series of dihydro-alkylthio-benzyl-oxopyrimidines (S-DABOs) bearing a 2-aryl-2-oxoethylsulfanyl chain at pyrimidine C2, an alkyl group at C5, and a 2,6-dichloro-, 2-chloro-6-fluoro-, and 2,6-difluoro-benzyl substitution at C6 (oxophenethyl-S-DABOs, 6-8) is here described. The new compds. showed low micromolar to low nanomolar (in one case subnanomolar) inhibitory activity against wt HIV-1. Against clin. relevant HIV-1 mutants (K103N, Y181C, and Y188L) as well as in enzyme (wt and K103N, Y181I, and L100I mutated RTs) assays, compds. carrying an ethyl/iso-Pr group at C5 and a 2,6-dichloro-/2...

[thiobarbiturat99]

Спасибо коллега. теперь подожду реаксис

[Chem_DM]

реаксис

[thiobarbiturat99]