• Archives of Pharmacal Research
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• v.16 no.1
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• pp.62-67
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• 1993

A series of 12 pyrimidine derivatives were prepared and tested in vitro against growth, sporulation and nucleic acids of Fusarium oxysporum f. sp. lycopersici and Helminthosporium oryzae. Intorduction of thiazole ring together with two aryl groups to 2-aminopyrimidine induced drastic toxicity for both fungi. Pyrimidine derivatives with aryl groups were less toxic. Nitro groups were found to enhance the toxicity of the pyrimidine derivatives especially when substituted in ortho-position of the aryl groups. Inhibition of nudeic acids synthesis of both fungi was attributed mainly to the presence of thiazole ring.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.217-222
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• 1995

Several acyclonucleoside analogues of pyrimidine base and N$^1$-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.

• Journal of the Korean Chemical Society
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• v.13 no.2
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• pp.177-180
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• 1969

5-Cyanopyrimidine derivatives were synthesized starting from 5-aminopyrimidine derivatives through the extended Sandmeyer reaction, and then these compounds were hydrolyzed to obtain pyrimidine-5-carboxylic acids. According to this procedure, 5-cyanopyrimidine derivatives and pyrimidine-5-carboxylic acid derivatives have been prepared in 62% and 65% yields, respectively, without any difficulties in removing impurities.

• Archives of Pharmacal Research
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• v.12 no.2
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• pp.103-107
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• 1989

Several new 1,2,4-triazolo[5,1-a]pyrimidine derivatives were synthesized via the reactions of 3-amino-1,2,4-triazole with active methylene nitrites and thier ylidene derivatives. The structures assigned for the reaction products were based on elemental analyses and spectral data.

• Journal of the Korean Chemical Society
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• v.60 no.4
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• pp.245-250
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• 2016

An improved protocol on the synthesis of thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives are reported. Previously, the thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives were prepared in a two-step procedure. Under the improved procedure, the thiazolo[3,2-a]pyrimidine-6-carboxylate derivatives was readily prepared in a one-step reaction. This procedure was found to be more efficient than the previous protocol and also compared to the ultrasound bath and conventional heating methods in terms of yield and reaction time.

• Journal of the Korean Chemical Society
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• v.39 no.9
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• pp.728-733
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• 1995

The derivatives of 2-amino-4-methylcyano-5-methylsulfonylpyrimidine 6 containing chloro, methoxy, ethoxy, phenoxy, amino and anilino groups at 6-position on the pyrimidine ring were prepared from 2-amino-4-chloro-5-methylsulfonylpyrimidine derivatives 4 and tert-butylcyanoacetate. The derivatives of 2-amino-4-chloro-5-methylsulfonylpyrimidine 4 containing methoxy, ethoxy, isopropoxy, phenoxy, amino and anilino groups at 6-position on the pyrimidine ring were prepared from 2-amino-4,6-dichloro-5-methylsulfonylpyrimidine 3.

• Archives of Pharmacal Research
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• v.20 no.4
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• pp.330-337
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• 1997

Thiocarboxamidocinnamonitrile derivatives 2 under bar a-f reacted with 3-aminopyrazole derivative 3 under bar a-c to give the pyrazole[3, 2-b]pyrimidine derivatives 6 under bar a-p. Compounds 6 under bar a-p were used as starting material for syntheses of several heterocylic coompounds. Dehydrogenation of 6 under bar gave pyrazole[3, 2-b]pyrimidines 10 under bar a-d while its reaction with diethyl oxalate gave 11 under bar. Reactions of 6 under bar with formic acid gave pyrazolopyrimidines 17 under bar a-j, and pyrazolopyrimidopyrimidines 18 under bar a-j.

• Journal of the Korean Chemical Society
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• v.54 no.6
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• pp.841-843
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• 2010

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.620-628
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• 1997

6-Aryl-5-cyano-4-pyrimidinon-2-thione derivatives 1a-c reacted with ethyl iodide to give the corresponded 2-S-ethylpyrimidin-4-one-derivatives 2a-c. Compounds 2a-c was, in turn, reacted with hydrazine hydrate to give the sulfur free reaction products, 3a-c. These reaction products were taken as the starting materials for the synthesis of several newly synthesized heterocyclic derivatives. Reactions with several halogenated ketones, esters, chloroacetic acid and chloroacetamide give pyrimidotriazines 8,12 and 15 while their reactions with formic acid, acetic acid and carbon disulfide gave the corresponded triazolopyrimidines 17 and 21. The reaction with both acetyl acetone and ethylacetoacetate gave the corresponded 2-$(3^{I},5^{I}-dimethyl-1^{I}-pyrazoly$pyrimidine derivatives 20a-c and 24a-c respectively while the reaction with cinnamonitriles 25a-h afforded the corresponded aryl hydrazopyrimidines 27a-f. The structure of these reaction products were eatablished based on both elemental anlayses and spectral data studies.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2627-2634
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• 2012

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel ${\beta}$-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, $^1H$ nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 ${\mu}g/mL$. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.