主权项 |
1. A process for preparing a polymer according to formula I: or a pharmaceutically acceptable salt, stereoisomer, isotopic variant or tautomer thereof; comprising the steps of A1) providing a compound of formula II: A2) reacting the compound of formula II with a polypeptide of formula III: to form the oxazolidine compound of formula IV: and A3) reacting the oxazolidine compound of formula IV with an acid to form the polymer of formula I; wherein AG is
a) a moiety comprising polyethylene glycol; or AG is -(L1-O)m-LINK-; LINK is an alkylene linker; the subscript m is an integer from 2-200; L1 is substituted or unsubstituted alkylene; and Y is hydroxy, protected hydroxyl, amino or protected amino; or Y is —O—R2, —O—C(O)—R2, —NH—C(O)—R2 or —NH—C(O)—O—R2;b) a biotin moiety; and Y is absent;c) a folate moiety; and Y is absent;d) a fluorescein moiety; and Y is absent;e) a lipid moiety; and Y is absent;f) a carbohydrate moiety; and Y is absent;g) a doxorubicin moiety; and Y is absent;h) a small molecule therapeutic moiety, wherein the small molecule therapeutic moiety comprises at least one carboxylic group; and Y is absent;i) a naproxen moiety; and Y is absent;j) an ibuprofen moiety; and Y is absent;k) a small molecule hormone moiety, wherein the small molecule hormone moiety comprises at least one carboxylic group; and Y is absent;l) a thyroxine moiety; and Y is absent; orm) a small molecule imaging agent moiety, wherein the small molecule imaging agent moiety comprises at least one carboxylic group; and Y is absent; X is hydroxyl, alkoxy, amino or substituted amino; R1 is H or methyl; each R2 is independently H, alkyl, or aryl; each R4 is independently H or substituted or unsubstituted alkyl; and the subscript t is 1, 2, 3, or 4. |