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US 6,291,673 B1Granted
Folic acid derivatives
AssigneePurdue Research Foundation
InventorsPhilip L. Fuchs, Jin Luo, Douglas A. Lantrip
Life of this patent
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Abstract
Novel folic acid derivatives and their use in preparation of γ-esters of folic acid via a pteroyl azide intermediate are described. Folic acid γ-esters are useful intermediates in the synthesis of folic acid conjugates capable of binding folate receptors in vitro and in vivo.
Claims2
A compound of the formula
- wherein Q is OH or NH2, Y is hydrogen, nitroso, C1-C4 alkyl, C1-C4 alkanoyl, C1-C4 halosubstituted alkanoyl and Z is NHNH2, or a group of formula
- provided that when Z is
- Y is other than acetyl or trifluroacetyl.
A method of preparing a compound of the formula
- wherein Q is OH or NH2, Y is hydrogen, nitroso, C1-C4 alkyl, C1-C4 alkanoyl, or C1-C4 halosubstituted alkanoyl, said method comprising the step of reacting a compound of formula
- wherein X is H or trifluroacetyl and Y′ is hydrogen, C1-C4 alkyl, C1-C4 alkanoyl or C1-C4 halosubstituted alkanoyl, with hydrazine.
Dependencies are inferred from the claim text.