Preparation of 5-amino-6-oxo-1,6-dihydro[1,2,4]triazine-3-carboxylic acid derivatives and synthesis of compound libraries thereof

Tetrahedron Letters

Volumn 45, Issue 13, 2004, Pages 2791-2795

  Gambert, Romain ^a   Kuratli, Christoph ^a   Martin, Rainer E ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

Combinatorial chemistry; Medicinal chemistry; Synthesis; Triazine

Indexed keywords

CARBOXYLIC ACID DERIVATIVE; TRIAZINE DERIVATIVE;

ARTICLE; CHEMICAL REACTION; DRUG SYNTHESIS; HYDROLYSIS; REACTION ANALYSIS; SOLUBILITY;

EID: 1542328783     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.tetlet.2004.02.025     Document Type: Article

References (13)

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6. +: 262.0940, found: 262.0944.
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9. +: 300.9895, found: 300.9900.
10. Compounds were purified by preparative HPLC on a Phenomenex Aqua 5 μm C18 125A 60 × 21.20 mm column equipped with a Gilson Liquid Handler 215 autosampler, two Varian Prep Star Model SD-1 pumps, a Sedex ELSD 75 lightscatter and a Dionex UVD 340S UV detector.
11. Solubility was measured from lyophilized DMSO stock solutions spectrophotometrically at pH=6.5 in a 0.05 M phosphate buffer.
12. logD values were measured spectrophotometrically at pH=7.4 in a 1-octanol/50 mM TAPSO buffer system containing 5% (v/v) DMSO.
13. a values were determined spectrophotometrically on a ProfilerSGA instrument in a SGA buffer system containing 10% (v/v) methanol at an ionic strength of 150 mM.