- An efficient and convenient synthesis of 4,6-Dichloro-2-methyl-5- nitropyrimidine
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A convenient synthesis of 4, 6-dihydro-2-methyl-pyrimidine can be obtained by cyclization reaction of acetamidine hydrochloride and diethyl malonate in the presence of sodium methoxide for a 91.2 % yield. 4, 6-Dihydro-2-methyl-5- nitropyrimidine can be achieved by nitration under the mixed acids of nitric acid, trichloroacetic acid and acetic acid in an 88.3 % yield and then the chlorination using phosphorus oxytrichloride can afford 4, 6-dichloro-2-methyl- 5-nitropyrimidine with an 82.6 % yield.
- Zhou, Shuwen,Xu, Defeng,Wang, Ziqiao,Zhu, Zhiling,Zha, Zhenyu,Fan, Yu,Su, Hongkui
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- Photochemical transformations of 4,6-dihydroxypyrimidine and 2-methyl-4,6-dihydroxypyrimidine isolated in low-temperature Ar, Ne and H2 matrices
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Monomers of 4,6-dihydroxypyrimidine and 2-methyl-4,6-dihydroxypyrimidine were trapped from the gas phase into low-temperature Ar, Ne and normal-H2 matrices. Dihydroxy and oxo-hydroxy tautomers were identified. The isolated monomers were exposed
- Rostkowska, Hanna,Luchowska, Anna,Lapinski, Leszek,Nowak, Maciej J.
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- Phenyl and Diaryl Ureas with Thiazolo[5,4-d]pyrimidine Scaffold as Angiogenesis Inhibitors: Design, Synthesis and Biological Evaluation
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Angiogenesis is crucial for tumor growth and inhibition of angiogenesis has been regarded as a promising approach for cancer therapy. Vascular endothelial growth factor receptor-2 (VEGFR-2) is an important factor in angiogenesis. In this work, a novel series of thiazolo[5,4-d]pyrimidine derivatives inhibiting angiogenesis were rationally designed and synthesized. Their inhibitory activities against human umbilical vein endothelial cells (HUVEC) were investigated in vitro. 1-(4-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19b) and 1-(3-Fluorophenyl)-3-{4-[(5-methyl-2-phenyl[1,3]thiazolo[5,4-d]pyrimidin-7-yl)amino]phenyl}urea (19g) exhibited the most potent inhibitory effect on HUVEC proliferation (IC50=12.8 and 5.3 μm, respectively). Compound 19g could inhibit the migration of human umbilical vein endothelial cells. These results support the further investigation of these compounds as potent anticancer agents.
- Xue, Wen-Jun,Deng, Ya-Hui,Yan, Zhong-Hui,Liu, Ji-Ping,Liu, Yu,Sun, Li-Ping
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- SUBSTANCES FOR DYEING KERATINOUS FIBERS
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Disclosed are substances which contain unsaturated, non-aromatic dialdehydes of formula (Ia) and/or the tautomer (Ib) thereof, wherein R1, R2, and R3 are defined as indicated in claim 1, along with at least one CH-acidic compound of formulas (II) and/or (III), wherein R6, R7, R8, R9, R10, Y, X?, Het, and X1 are defined as indicated in claim 1, in a cosmetic carrier. Said substances color keratinous fibers, especially human hair, in an intensive, colorfast, natural brown shade.
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- A convenient synthesis of 5-arylamino-4H-pyran-4-ones using palladium-catalyzed amination
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A concise approach to 5-arylamino-4H-pyran-4-ones is described via palladium-catalyzed amination reaction. The methodology involved in this Letter is based on protection/deprotection protocols and on manipulation of the 5-hydroxy group of readily available kojic acid. It would provide a new entry to a range of 5-arylamino-4H-pyran-4-ones via Buchwald-Hartwig-type amination reaction on 4H-pyran-4-one unit.
- Farard, Julien,Logé, Cédric,Pfeiffer, Bruno,Lesur, Brigitte,Duflos, Muriel
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scheme or table
p. 5729 - 5732
(2009/12/09)
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- Pyrimidine derivatives
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The present invention relates to novel 5-(ω-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.
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- Antihypertensive Activity of 6-Arylpyridopyrimidin-7-amine Derivatives
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A series of 51 6-arylpyridopyrimidin-7-amine derivatives was prepared and evaluated for antihypertensive activity in the conscious spontaneously hypertensive rat.A number of these compounds, notably 6-(2,6-dichlorophenyl)-2-methylpyridopyrimidin-7-amine (36), lowered blood pressure in these rats in a gradual and sustained manner to normotensive levels at oral doses of 10-50 mg/kg.Normalized blood pressure levels could then be maintained by single daily oral doses.The effect of structural variation in the 6-aryl group and in the 2 and 4 positions of the pyridopyrimidine ring on activity is reported and discussed.
- Bennett, Lawrence R.,Blankley, C. John,Fleming, Robert W.,Smith, Ronald D.,Tessman, Deirdre K.
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p. 382 - 389
(2007/10/02)
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