Click chemistry, a powerful tool for pharmaceutical sciences

Christopher D. Hein, Xin Ming Liu, Dong Wang

Research output: Contribution to journalReview articlepeer-review

645 Scopus citations


Click chemistry refers to a group of reactions that are fast, simple to use, easy to purify, versatile, regiospecific, and give high product yields. While there are a number of reactions that fulfill the criteria, the Huisgen 1,3-dipolar cycloaddition of azides and terminal alkynes has emerged as the frontrunner. It has found applications in a wide variety of research areas, including materials sciences, polymer chemistry, and pharmaceutical sciences. In this manuscript, important aspects of the Huisgen cycloaddition will be reviewed, along with some of its many pharmaceutical applications. Bioconjugation, nanoparticle surface modification, and pharmaceutical-related polymer chemistry will all be covered. Limitations of the reaction will also be discussed.

Original languageEnglish (US)
Pages (from-to)2216-2230
Number of pages15
JournalPharmaceutical Research
Issue number10
StatePublished - Oct 2008


  • Bioconjugation
  • Click chemistry
  • Drug delivery
  • Nanomedicine
  • Polymer

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)


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