First Scale-Up to Production Scale of a Ring Closing Metathesis Reaction Forming a 15-Membered Macrocycle as a Precursor of an Active Pharmaceutical Ingredient

Artigo Revisado por pares

First Scale-Up to Production Scale of a Ring Closing Metathesis Reaction Forming a 15-Membered Macrocycle as a Precursor of an Active Pharmaceutical Ingredient

2005; American Chemical Society; Volume: 9; Issue: 4 Linguagem: Inglês

10.1021/op0580015

ISSN

1520-586X

Autores

Thomas Nicola, Michael Brenner, Kai Donsbach, Paul Kreye,

Tópico(s)

HIV/AIDS drug development and treatment

Resumo

BILN 2061 ZW (4) is a new chemical entity which shows promising results against the Hepatitis C virus. The major issue in the synthetic route represents the scale-up of a ring closing metathesis reaction to form a 15-membered macrocycle. The parameters chosen for the macrocyclization are discussed, and the experience during large scale synthesis, trouble shooting, and possible improvements for future campaigns are described.

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First Scale-Up to Production Scale of a Ring Closing Metathesis Reaction Forming a 15-Membered Macrocycle as a Precursor of an Active Pharmaceutical Ingredient