Method for the preparation of 1-benzotriazolyl carbonate...

C - Chemistry – Metallurgy – 08 – G

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C08G 65/333 (2006.01) A61K 47/48 (2006.01) C08G 65/329 (2006.01) C08G 65/332 (2006.01)

Patent

CA 2393638

The invention provides a method for preparing a 1-benzotriazolylcarbonate ester of a water-soluble and non-peptidic polymer by reacting a terminal hydroxyl group of a water-soluble and non- peptidic polymer with di(1-benzotriazolyl)carbonate in the presence of an amine base and an organic solvent. The polymer backbone can be poly(ethylene glycol). The 1-benzotriazolylcar-bonate ester can then be reacted directly with a biologically active agent to form a biologically active polymer conjugate or reacted with an amino acid such as lysine, to form an amino acid derivative.

Cette invention a trait à un procédé de préparation d'un ester de 1-benzotriazolylcarbonate d'un polymère hydrosoluble et non peptidique par réaction d'un groupe hydroxy terminal d'un polymère hydrosoluble et non peptidique avec un di(1-benzotriazolyl)carbonate en présence d'une base amine et d'un solvant organique. Le squelette polymère peut être un poly(éthylène glycol). Il est possible de faire réagir directement l'ester de 1-benzotriazolylcarbonate avec un agent biologiquement actif afin de former un conjugué polymère biologiquement actif ou bien de le faire réagir avec un acide aminé tel que la lysine et ce, afin de former un dérivé aminoacide.

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