| 摘要 |
PURPOSE: Novel Knoevenagel condensation products, methods for their production and their use for pharmaceutical and analytical purposes are provided. Further, conjugates between the Knoevenagel condensates and biomolecules are provided. CONSTITUTION: (Z)-5'-O-phosphonopyridoxylidenrodanine of formula(3), the representative compound of derivatives of vitamin B6 coenzyme pyridoxal 5'-phosphate of formula(1), is prepared to provide novel compounds suitable for pharmaceutical and analytical use. Knoevenagel condensation between the compound of formula(1) and synthetic susceptible compound, rodanine of formula(2) gives the compound of formula(3). The compound of formula(3) includes (Z)-5-££5-hydroxy-6-methyl-3-£(phophonoxy)methyl|-4-pyridyl|methylene|2-thioxo-4-thia zolidinone. In the compound of formula(3), rodanine group can bind biomolecules such as single-stranded nucleic acid, and electrically charged phosphate group has good water solubility. Derivatives of the compound of formula(3) are obtained by using C12-C18 fatty acyl chloride to OH group thereof. Additionally, the invention includes compounds of formula(8); their salts, for example, alkali metal salts, alkali earth metal salts or ammonium salts; their hydrates; and their stereoisomers. Knoevenagel condensation between compounds of formula(9) and compounds of formula(10) gives the compounds of formula(8).
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