- A green and facile synthesis of 6-Methyl-2-(alkylthio)pyrimidin-4(3H)-one
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Reaction of 2-thiouracil (1) with alkylating agents, namely dimethyl sulphate, diethyl sulphate and benzyl chloride in the presence of potassium carbonate as a mild base, under green conditions, such as simple physical grinding of reactants or in solvents such as ethanol and PEG-600 and under microwave irradiation, gave, respectively 6-methyl-2-(methylthio)pyrimidin-4(3H) -one (2a, i.e., R=CH3), 6-methyl-2-(ethylthio) pyrimidin-4(3H)-one (2b, i.e., R = C2H5) and 6-methyl-2-(benzylthio)pyrimidin- 4(3H)-one (2c, i.e., R = PhCH2Cl). Alternately, condensation of ethyl acetoacetate with S-methylisothiouronium hemisulfate, S-ethylisothiouronium hemisulfate and S-benzyl isothiouronium chloride in ethanolic potassium hydroxide under reflux for 3 h gave 2a-c respectively.
- Kotaiah,Ramadevi,Naidu,Dubey
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- Studies on solubility and S-alkylation of 2-thiouracil in ionic liquids
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Ionic liquids have been exploited to assist dissolution of poorly soluble (and poorly bioavailable) drugs, enhancing permeation through physiological barriers to deliver drugs to target sites. Herein, the solubility of 6-methyl-2-thiouracil – a common ant
- Nestor, Stephen T.,Hawkins, Allison N.,Xhani, Xhensila,Sykora, Richard E.,Mao, James X.,Nam, Kwangho,McManus, Gregory J.,Mirjafari, Arsalan
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- HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
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Paragraph 00183
(2016/10/31)
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- HEPATITIS B VIRAL ASSEMBLY EFFECTORS
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Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.
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Paragraph 00137; 00138
(2015/05/05)
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- Exploring the scope for scale-up of organic chemistry using a large batch microwave reactor
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A new batch microwave reactor has been evaluated in the context of palladium-mediated transformations, condensation reactions, nucleophilic aromatic substitution reactions, and alkylations. Importantly, a linear scaling approach was taken, no changes being made to the protocol when moving from the small, developmental scale to larger scales. In some cases reactions were scaled over 18,000-fold when moving from small (0.1-1 mmol) to large (1-18 mol) runs.
- Schmink, Jason R.,Kormos, Chad M.,Devine, William G.,Leadbeater, Nicholas E.
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experimental part
p. 205 - 214
(2010/04/29)
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- Synthesis and antimicobacterial activity of 2-substituted 4-arylamino-6-methylpyrimidines
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2-Substituted 4-arylamino-6-methylpyrimidines were synthesized by stepwise modification of the structure of 6-methyl-2-thiouracyl through the intermediate 2-(ar)alkylthio-6-methyl-4-chloropyrimidines. Some of the compounds synthesized exhibit expressed antimycobacterial activity.
- Erkin,Krutikov,Smirnova
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experimental part
p. 1944 - 1948
(2009/02/08)
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- Special features of the nucleophilic substitution of halogen in alkyl and benzyl halides with anions generated from 4-hydroxy-2-mercapto-6- methylpyrimidine
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The nucleophilic substitution of halogen (chlorine, bromine, and iodine) in alkyl and benzyl halides has been effected in aqueous dioxane media with S-and O-anions generated from 4-hydroxy-2-mercapto-6-methylpyrimidine. Under these conditions replacement
- Rakhimov,Titova,Fedunov,Babkin, Vladimir Aleksandrovich
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experimental part
p. 700 - 708
(2009/04/06)
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- Synthesis of 2-alkyl(aralkyl)sulfanyl-6-methylpyrimidin-4(3H)-ones and 4-alkyl(aralkyl)oxy-2-alkyl(aralkyl)sulfanyl-6-methylpyrimidines
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2-Alkyl(aralkyl)sulfanyl-6-methylpyrimidin-4(3H)-ones and 4-alkyl(aralkyl)oxy-2-alkyl(aralkyl)-sulfanyl-6-methylpyrimidines having similar or different substituents on the sulfur and oxygen atoms were synthesized by alkylation of sodium salts derived from
- Rakhimov,Titova
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