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Multi-Kilo Delivery of AMG 925 Featuring a Buchwald-Hartwig Amination and Processing with Insoluble Synthetic Intermediates

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Amgen describes the development of a synthetic route to manufacture the drug candidate AMG 925 on kilogram scale. The synthetic route features a Buchwald-Hartwig amination using BrettPhos as ligand and conducted to afford 12 kg of product in a single batch (scheme).

Yet, the target levels of heavy metal in the drug substance AMG 925 were < 100 ppm, much lower than that found in the crude Buchwald-Hartwig product (700 - 800 ppm).

After the screening of potential scavengers, SiliaMetS Thiourea was selected as the scavenger of choice since it was the most effective. At 100 wt % relative to crude product, in 80 % (v/v) toluene/MeOH and a total of 15 volumes of solvent, it afforded product in 90 % with less than 2 ppm of residual Pd.

Caille, S. et al. Org. Process Res. Dev., 2015, 19, 476 - 485

 

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  1. SiliaMetS Thiourea (THU) (R69530B)

    SiliaMetS Thiourea (THU) (R69530B)

    SiliaMetS Thiourea (Si-THU) is a versatile metal scavenger for all forms of palladium, and is widely used in the pharmaceutical industry. Once complexed with a transition metal, it has also been reported as being an effective catalyst. Best scavenger for: Pd & Ru. Good scavenger for: Ag, Cu, Fe, Os, Rh, Sc & Sn.

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