Designing Efficient Cascade Reactions in Drug Discovery

Chenguang Yu, He Huang, Chunquan Sheng, Wei Wang

Research output: Chapter in Book/Report/Conference proceedingChapter

1 Scopus citations


This chapter focuses on the exploration and application of cascade reactions in the total synthesis of both biologically active natural products and their analogues and synthetic substances for drug discovery. The high synthetic efficiency of such processes enables the facile and rapid construction of bioactive molecules and furthermore streamlines the study of structure-activity relationships to accelerate the identification of potential drug-like compounds for further biological evaluation. In addition, the power of cascade strategies is also demonstrated in the pilot plant-scale synthesis of highly valued, structurally complex drugs and drug candidates.

Original languageEnglish (US)
Title of host publicationMethods in Pharmacology and Toxicology
PublisherHumana Press Inc.
Number of pages23
StatePublished - 2022

Publication series

NameMethods in Pharmacology and Toxicology
ISSN (Print)1557-2153
ISSN (Electronic)1940-6053


  • Cascade reaction
  • Drug discovery and development
  • Organocatalysis
  • Pilot plant-scale synthesis
  • Structure-activity relationships
  • Transition metal catalysis

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Pharmacology (medical)


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