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US 7,411,031 B2Granted
Synthesis of polyanhydrides
AssigneeRutgers, The State University of New Jersey
InventorsKathryn E. Uhrich, Robert C. Schmeltzer, Theodore James Anastasiou
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Abstract
The present invention provides a method for forming compounds of Formula HO—C(═O)R1—X—R2—X—R1—C(═O)—O—H wherein compound (I) can be polymerized to provide a polymer that contains therapeutically active compounds. In the compounds of the invention, each R1 is group that will provide the therapeutically active compound upon hydrolysis of the polymer; each X is independently an ester linkage or an amide linkage; and R2 is a linking group.
Claims26
A process for preparing a compound having Formula (I)
- HO—C(═Y)R1—X—R2—X—R1—C(═Y)—OH (I)
- wherein each R1 is an organic group;
- each Y is independently O or S;
- each X is independently an ester linkage, an amide linkage, a thioester linkage or a thioamide linkage;
- and R2 is a linking group;
- comprising reacting a compound of Formula (II)
- R3—R1—C(═O)OH (II)
- with a compound of Formula (III)
- X2—C(═Y)—R2—C(═Y)—X2 (III)
- wherein R3 is an hydroxy, amine, or thiol group or an organic radical comprising an hydroxy, amine, or thiol group;
- and each X2 is a halogen;
- in the presence of at least 2 equivalents to about 50 equivalents of an organic base;
- optionally in a suitable solvent.
10 more elements
Dependencies are inferred from the claim text.