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Macrocyclic Chemistry

Whether a macrocycle program can actually be supplied, rather than only demonstrated.

The platform

We construct versatile macrocyclic compounds and have applied more than 10 representative cyclization methods, covering lactams, lactones, sulfonamides, ethers, and bicyclic and tricyclic structures. 

  • More than 18 years of experience 
  • More than 2,000 macrocyclic compounds synthesized 
  • More than 50 g of desired product obtained through a synthesis of 20 to 31 steps 
  • More than 10 representative cyclization methods

Cyclization methods

  • Mitsunobu cyclization 
  • Ring-closing metathesis 
  • Sulfonamide formation 
  • Lactam cyclization 
  • Substitution cyclization 
  • Click reaction 
  • Reductive amination 
  • C–H activation 
  • Disulfide bond formation 

The honest measure

Any laboratory can close a ring once. Delivering more than 50 grams through a 20 to 31 step sequence is the number that tells you whether the program can be supplied through toxicology and into the clinic.

Discovery Process Chemistry
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