Methods of preparing activated polymers having alpha nitrogen groups
AssigneeEnzon Pharmaceuticals, Inc.
InventorsHong Zhao, Dechun Wu
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Abstract
Methods for preparing substantially non-antigenic polymers having lone electron pair-containing moieties in high purity are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed. The resultant polymer-amines are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.
Claims27
A method of preparing a polymer having a lone electron pair-containing moiety thereon, comprising:
- reacting a polymer of formula (I)
- R2-R1-(L1)n-LG (I)
- wherein
- R1 is a substantially non-antigenic polymer;
- R2 is a capping group, LG or LG-(L1)n-;
- L1 is a bifunctional linker;
- LG is a leaving group;
- and
- n=0 or positive integer,
- with a compound having a lone electron pair-containing group thereon in an aqueous base at a temperature of from about 10 to about 80° C. and for a reaction time of less than about 24 hours.
The method of claim 6, wherein LG is
Dependencies are inferred from the claim text.