Narcistatin prodrugs
First Claim
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1. A method for synthesizing pyridinium narcistatin, comprising reacting:
- narciclasine;
tetrabutylammonium dihydrogen phosphate;
dicyclohexylcarbodiimide; and
p-toluenesulfonic acid in pyridine, to form a reaction mixture and forming pyridinium narcistatin.
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Abstract
The present invention provides prodrugs derived from the sparingly soluble anticancer isocarbostyril narciclasine, a component of various Narcissus species, said prodrugs having potential for use against animal and human cancers. Also disclosed is an efficient procedure for the synthetic conversion of narciclasine to several more soluble cyclic phosphate compounds, including “narcistatin”.
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10 Claims
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1. A method for synthesizing pyridinium narcistatin, comprising reacting:
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narciclasine; tetrabutylammonium dihydrogen phosphate; dicyclohexylcarbodiimide; and p-toluenesulfonic acid in pyridine, to form a reaction mixture and forming pyridinium narcistatin. - View Dependent Claims (2)
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3. A method for synthesizing pyridinium narcistatin, comprising reacting
narciclasine; -
tetrabutylammonium dihydrogen phosphate; and dicyclohexylcarbodiimide in pyridine, to form a reaction mixture and forming pyridinium narcistatin. - View Dependent Claims (4)
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- 5. A method for synthesizing a compound having the formula:
- 8. A method for synthesizing a compound having the formula:
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