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Macrocyclization via Ring-Closing Metathesis in Drug Discovery & Process Chemistry

Drug Hunter

Interestingly, among the six case studies, none use the well-known Hoveyda-Grubbs II (HG-II) catalyst in the largest scale synthesis disclosed, though several employ HG-II derivatives, highlighting the rapid evolution of catalytic methods and distinct considerations for process chemistry. Gonzalez-Bobes, F. 2023 , 66 , (8), 5377-5396.

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Metabolism of macrocyclic drugs

Metabolite Tales Blog

Synthetic macrocycles in oncology Pactritinib is a multi-kinase JAK2/FLT3 inhibitor used for the treatment of primary and secondary myelofibrosis, approved by the FDA in 2022. Journal of Medicinal Chemistry, 66 (8), 5377-5396. Journal of Medicinal Chemistry 62 (21), 9418-9437. Ayushi Jain and Khalid Mumtaz, 2022.

Drugs 52
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Metabolism of de novo designed macrocyclic drugs

Metabolite Tales Blog

Synthetic macrocycles in oncology Pactritinib is a multi-kinase inhibitor used for the treatment of primary and secondary myelofibrosis and was approved by the FDA in 2022. Journal of Medicinal Chemistry, 66 (8), 5377-5396. Journal of Medicinal Chemistry 62 (21), 9418-9437. Ayushi Jain and Khalid Mumtaz, 2022. Chen et al.,