Boyer Cyrille, Bulmus Volga, Davis Thomas P
Centre for Advanced Macromolecular Design (CAMD), School of Chemical Sciences and Engineering, The University of New South Wales, Sydney NSW 2052 Australia.
Macromol Rapid Commun. 2009 Apr 1;30(7):493-7. doi: 10.1002/marc.200800708. Epub 2009 Feb 12.
End group modification of polymers prepared by reversible addition-fragmentation chain transfer (RAFT) polymerization was accomplished by conversion of trithiocarbonate into reactive functions able to conjugate easily with biomolecules or bioactive functionality. Polymers were prepared by RAFT, and subsequent aminolysis led to sulfhydryl-terminated polymers that reacted in situ with an excess of dithiopyridyl disulfide to yield pyridyl disulfide-terminated macromolecules or in the presence of ene to yield functional polymers. In the first route, the pyridyl disulfide end groups allowed coupling with oligonucleotide and peptide. The second approach exploited thiol-ene chemistry to couple polymers and model compounds such as carbohydrate and biotin with high yield.
通过可逆加成-断裂链转移（RAFT）聚合制备的聚合物的端基修饰是通过将三硫代碳酸酯转化为能够与生物分子或生物活性官能团轻松共轭的反应性功能来实现的。聚合物通过RAFT制备，随后的氨解反应生成巯基封端的聚合物，该聚合物与过量的二硫代吡啶二硫化物原位反应，生成吡啶二硫化物封端的大分子，或者在烯存在的情况下生成功能聚合物。在第一条路线中，吡啶二硫化物端基允许与寡核苷酸和肽偶联。第二种方法利用硫醇-烯化学以高产率将聚合物与模型化合物（如碳水化合物和生物素）偶联。
