- Process for synthesis of cytosine
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The invention discloses a process for synthesizing cytosine. A 3-hydroxyacrylonitrile compound and an O-methylisourea compound or an S-methylisothiourea compound or an S-ethylisothiourea compound or an S-benzylisothiourea compound are used as raw materials. The process comprises the steps of adding a catalyst and an organic solvent into a reaction kettle, stirring, and then adding the raw materials; heating the mixture to be 50-90 DEG C, and reacting for 8-12 hours; evaporating the solvent to obtain an intermediate; adding concentrated hydrochloric acid into the intermediate, heating to be 70-100 DEG C, and preserving the heat for 1-2 hours; adding water, performing hot filtration, and cooling the obtained filtrate to room temperature; dripping a sodium hydroxide solution into the filtrate to adjust the pH value to be 7-7.5, and cooling to 10-15 DEG C; filtering after cooling, washing, and drying to obtain the cytosine. The process has the advantages that the process steps are simple, the production period is short, and the cost is low; the conversion rate of the raw materials is high, and the synthesized product is good in quality and high in yield, so that the process is suitable for industrialized production.
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Paragraph 0010; 0021
(2017/05/05)
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- Peptide deformylase inhibitors
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
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Page/Page column
(2014/12/09)
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- PEPTIDE DEFORMYLASE INHIBITORS
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The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
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Page/Page column
(2014/02/15)
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- Highly efficient, chemoselective syntheses of 2-methoxy-4-substituted pyrimidines
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Three 2-methoxy-4-substituted pyrimidine compounds were chemoselectively synthesized by diazotization, using 2,4-dichloropyrimidine as the starting material. In nonaqueous diazotization reaction system, halo-substituted 6 and 7 were efficiently prepared, and in aqueous medium, hydrolysis product 8 was afforded.
- Xu, Chunyan,Cheng, Chuanjie,Liu, Hongtao,Liu, Bo
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scheme or table
p. 545 - 548
(2012/06/01)
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- PYRIMIDINE DERIVATIVES
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A compound of the following formula: wherein R1, R2, R3, R4, R5,T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.
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Page/Page column 65
(2008/12/04)
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- 5,7-DIAMINOPYRAZOLO [4,3-d] PYRIMIDINES WITH PDE-5 INHIBITING ACTIVITY
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This invention relates to compounds of formula (I).
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Page/Page column 80
(2008/06/13)
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- Asymmetric synthesis of 2'-phosphonomethyl(3',4'-dihydroxybutyl)cytosine and -guanine nucleotides
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The synthesis of 2'-phosphonomethyl(3',4'-dihydroxylbutyl) nucleotides of cytosine and guanine 13 and 15 possessing the 2'S,3'S absolute configuration was readily accomplished in eleven and ten steps respectively from L-ascorbic acid via the protected tetrols 9 and 8. Alcohol 8 undergoes efficiently a regiospecific Mitsunobu coupling with 6-chloro-2-aminopurine to furnish the N-9 isomer which was further transformed to 15.
- Evans, Colleen A.,Hewgill, Randolph T.,Mansour, Tarek S.
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p. 2299 - 2302
(2007/10/03)
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- Fluorinated Heterocyclic Compounds. 2. 2,4-Difluoro and 4-Amino-2-fluoropyrimidines, Nucleoside Base Analogs
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Nucleoside base analogs in which fluoro substituents replace the enolic hydroxy groups of uracil, thymine and cytosine have been prepared.Improved methods for the preparation and isolation of the known 2,4-difluoropyrimidine, 2,4-difluoro-6-methylpyrimidine and the new 2,4-difluoro-5-methylpyrimidine, 2-fluoro-4-aminopyrimidine, 4-fluoro-2-aminopyrimidine, and other alkylaminofluoropyrimidines are described.
- Svirskaya, Polina I.,Yedidia, Varda,Leznoff, Clifford C.,Miller, Jack M.
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p. 149 - 153
(2007/10/02)
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- Method of preparing 2-alkoxy-4-aminopyrimidines
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2-Alkoxy-4-aminopyrimidines, having if desired a substituent in position 5, are prepared from 4-amino-2-carboxymethylthiopyrimidines by conversion with alcohols in the presence of bases.
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- Studies on Nucleosides and Nucleotides. VIII. Preparation and Reactions of Triphenylphosphoranediylnucleosides
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The reaction of uridine, N4-benzoylcitidine, guanosine, and N6-p-toluoyladenosine with diethyl azodicarboxylate and triphenylphosphine resulted in the formation of the corresponding 2',3'-O-(triphenylphosphoranediyl)cyclonucleosides.On the other hand, adenosine afforded, under similar conditions, 3',5'-O-(triphenylphosphoranediyl)adenosine (19).The difference can be explained in terms of the acidity of base moieties of the nucleosides.The reaction of 2',3'-O-(triphenylphosphoranediyl)-O2,5'-cyclouridine, N4-benzoyl-2',3'-O-(triphenylphosphoranediyl)-O2,5'-cyclocytidine, 2',3'-O-(triphenylphosphoranediyl)-N3,5'-cycloguanosine, or N6-p-toluoyl-2',3'-O-(triphenylphosphoranediyl)-N3,5'-cycloadenosine with nucleophiles and with electrophiles addorded the corresponding nucleoside derivatives with free 2'- and 3'-hydroxyl groups.Thus the 2',3'-O-triphenylphosphoranediyl group serves as a protecting group which is readily removed during work-up of the reaction products. 19 reacted with phenyl isocyanate to give 5'-O-phenylcarbamoyladenosine and N6,5'-O-bis(phenylcarbamoyl)adenosine.The reaction of 19 with diphenylketene also afforded acyladenosines with free 2'- and 3'-hydroxyl groups.These results suggested that 3',5'-O-triphenylphosphoranediyl group activates the 5'-carbon atom of adenosine.
- Kimura, Junji,Yagi, Kentaro,Suzuki, Hideyuki,Mitsunobu, Oyo
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p. 3670 - 3677
(2007/10/02)
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