Acylbenzotriazoles: New Allies for Short Linear and Cyclic Peptide Constructs

  • Danniebelle N. HaaseEmail author
Part of the Topics in Heterocyclic Chemistry book series (TOPICS, volume 43)


Peptides and proteins have tremendous potential as medicinal drugs, but their potential has largely been untapped due to several problems such as their fast degradation by enzymes and limited bioavailability. Major advances in the development of peptide synthesis methods, availability of a wide array of coupling reagents and other augments have lowered the barrier to entry for peptide drugs. However, greater access to peptides and proteins is needed in order to realize the possibilities for diagnosing, treating and monitoring critical diseases. Acylbenzotriazoles are an expedient gateway to cyclic and difficult peptides. With this overview, we now describe the use of acylbenzotriazoles as allies for the construction of peptides and peptide conjugates. The efficacy of N-(protected-α aminoacyl)benzotriazoles for the preparation of an extensive range of enantiopure peptides with good yields and purities on solid-phase or in solution, as well as challenges encountered and the way forward is addressed in the chapter.


Acylbenzotriazole Amino acids Isopeptide Microwave Peptide synthesis Peptides Solid-phase 


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Copyright information

© Springer International Publishing Switzerland 2016

Authors and Affiliations

  1. 1.The Dow Chemical CompanyCollegevilleUSA

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